Spirocycle integrin inhibitors

ABSTRACT

This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-   8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the α v  β 3  integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

FIELD OF THE INVENTION

This application claims priority under 35 U.S.C. § 119(e) from provisional application Ser. No. 60/013,539, filed Mar. 15, 1996.

This invention relates to novel heterocycles which are useful as antagonists of the α_(v) β₃ integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

BACKGROUND OF THE INVENTION

Angiogenesis or neovascularization is critical for normal physiological processes such as embryonic development and wound repair (Folkman and Shing, J. Biol. Chem. 1992, 27:10931-10934; D'Amore and Thompson, Ann. Rev. Physiol. 1987, 49:453-464). However, angiogenesis also occurs pathologically, for example, in ocular neovascularization (leading to diabetic. retinopathy, neovascular glaucoma, retinal vein occlusion and blindness), in rheumatoid arthritis and in solid tumors (Folkman and Shing, J. Biol. Chem., 1992, 267:10931-10934; Blood and Zetter, Biochim. Biophys. Acta., 1990, 1032:118-128).

Tumor dissemination, or metastasis, involves several distinct and complementary components, including the penetration and transversion of tumor cells through basement membranes and the establishment of self-sustaining tumor foci in diverse organ systems. To this end, the development and proliferation of new blood vessels, or angiogenesis, is critical to tumor survival. Without neovascularization, tumor cells lack the nourishment to divide and will not be able to leave the primary tumor site (Folkman and Shing, J. Biol. Chem., 1992, 267:10931-10934).

Inhibition of angiogenesis in animal models of cancer has been shown to result in tumor growth suppression and prevention of metastatic growth (Herblin et al., Exp. Opin. Ther. Patents, 1994, 1-14). Many angiogenic inhibitors have been directed toward blocking initial cytokine-dependent induction of new vessel. growth, e.g. antibodies to endothelial cell growth factors. However, these approaches are problematic because tumor and inflammatory cells can secrete multiple activators of angiogenesis (Brooks et al., Cell, 1994, 79:1157-1164). Therefore, a more general approach that would allow inhibition of angiogenesis due to a variety of stimuli would be of benefit.

The integrin α_(v) β₃ is preferentially expressed on angiogenic blood vessels in chick and man (Brooks et al., Science, 1994, 264:569-571; Enenstein and Kramer, J. Invest. Dermatol., 1994, 103:381-386). Integrin α_(v) β₃ is the most promiscuous member of the integrin family, allowing endothelial cells to interact with a wide variety of extracellular matrix components (Hynes, Cell, 1992, 69:11-25). These adhesive interactions are considered to be critical for angiogenesis since vascular cells must ultimately be capable of invading virtually all tissues.

While integrin α_(v) β₃ promotes adhesive events important for angiogenesis, this receptor also transmits signals from the extracellular environment to the intracellular compartment (Leavesley et al., J. Cell Biol., 1993, 121:163-170, 1993). For example, the interaction between the α_(v) β₃ integrin and extracellular matrix components promotes a calcium signal required for cell motility.

During endothelium injury, the basement membrane zones of blood vessels express several adhesive proteins, including but not limited to von Willebrand factor, fibronectin, and fibrin. Additionally, several members of the integrin family of adhesion receptors are expressed on the surface of endothelial, smooth muscle and on other circulating cells. Among these integrins is α_(v) β₃ the endothelial cell, fibroblast, and smooth muscle cell receptor for adhesive proteins including von Willebrand factor, fibrinogen (fibrin), vitronectin, thrombospondin, and osteopontin. These integrins initiate a calcium-dependent signaling pathway that can lead to endothelial cell, smooth muscle cell migration and, therefore, may play a fundamental role in vascular cell biology.

Recently, an antibody to the α_(v) β₃ integrin has been developed that inhibits the interaction of this integrin with agonists such as vitronectin (Brooks et al., Science, 1994, 264:569-571). Application of this antibody has been shown to disrupt ongoing angiogenesis on the chick chorioallantoic membrane (CAM), leading to rapid regression of histologically distinct human tumor transplanted onto the CAM (Brooks et al., Cell, 1994, 79:1157-1164). In this model, antagonists of the α_(v) β₃ integrin induced apoptosis of the proliferating angiogenic vascular cells, leaving pre-existing quiescent blood vessels unaffected. Thus, α_(v) β₃ integrin antagonists have been shown to inhibit angiogenesis and are recognized as being useful as therapeutic agents for the treatment of human diseases such as cancer, restenosis, thromoembolic disorders, rheumatoid arthritis and ocular vasculopathies (Folkman and Shing, J. Biol. Chem., 1992, 267:10931-10934).

Increasing numbers of other cell surface receptors have been identified which bind to extracellular matrix ligands or other cell adhesion ligands thereby mediating cell-cell and cell-matrix adhesion processes. These receptors belong to a gene superfamily called integrins and are composed of heterodimeric transmembrane glycoproteins containing α- and β-subunits. Integrin subfamilies contain a common β-subunit combined with different α-subunits to form adhesion receptors with unique specificity. The genes for eight distinct β-subunits have been cloned and sequenced to date.

The α_(v) β₃ heterodimer is a member of the β₃ integrin subfamily and has been described on platelets, endothelial cells, melanoma, smooth muscle cells, and osteoclasts (Horton and Davies, J. Bone Min. Res. 1989, 4:803-808; Davies et al., J. Cell. Biol. 1989, 109:1817-1826; Horton, Int. J. Exp. Pathol., 1990, 71:741-759). Like GPIIb/IIIa, the vitronectin receptor binds a variety of RGD-containing adhesive proteins such as vitronectin, fibronectin, VWF, fibrinogen, osteopontin, bone sialo protein II and thrombosponden in a manner mediated by the RGD sequence. A key event in bone resorption is the adhesion of osteoclasts to the matrix of bone. Studies with monoclonal antibodies have implicated the α_(v) β₃ receptor in this process and suggest that a selective α_(v) β₃ antagonist would have utility in blocking bone resorption (Horton et al., J. Bone Miner. Res., 1993, 8:239-247; Helfrich et al., J. Bone Miner. Res., 1992, 7:335-343).

PCT Patent Application Publication Number WO95/14683, published Jun. 1, 1995 discloses isoxazoline and isoxazole fibrinogen receptor antagonists of general formula shown below: ##STR1##

Copending, commonly assigned U.S. patent application Ser. No. 08/455,768 filed May 31, 1995. discloses integrin inhibitors of the general formula shown below: ##STR2##

PCT Patent Application Publication No. WO95/32710, published Dec. 7, 1995 discloses compounds for inhibition of osteoclast-mediated bone resorption of general formula shown below:

    X--Y--Z--Aryl--A--B

wherein Aryl is a 6-membered aromatic ring system.

None of the above references discloses or suggests the spirocyclic compounds of the present invention which are described in detail below.

SUMMARY OF THE INVENTION

The present invention provides novel nonpeptide compounds which bind to integrin receptors thereby altering cell-matrix and cell-cell adhesion processes. The compounds of the present invention are useful for the inhibition of cell adhesion and the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

One aspect of this invention provides novel compounds of Formula I (described below) which are useful as antagonists of the α_(v) β₃ integrin, which is also referred to as the vitronectin receptor. The compounds of the present invention inhibit the binding of vitronectin or other RGD-containing ligands to α_(v) β₃ and inhibit cell adhesion. The present invention also includes pharmaceutical compositions containing such compounds of Formula I, and methods of using such compounds for the inhibition of angiogenesis, and/or for the treatment of disorders mediated by angiogenesis.

Another aspect of the present invention comprises agents that inhibit the binding of vitronectin to the α_(v) β₃ receptor for the treatment (including prevention) of thrombosis which do not significantly alter hemostatic balance and do not significantly inhibit platelet aggregation and do not significantly inhibit coagulation. Also the compounds of the current invention can be used for the treatment or prevention of restenosis.

The present invention also provides novel compounds, pharmaceutical compositions and methods which may be used in the treatment or prevention of other diseases which involve cell adhesion processes, including, but not limited to, rheumatoid arthritis, asthma, allergies, adult respiratory distress syndrome, graft versus host disease, organ transplantation, septic shock, psoriasis, eczema, contact dermatitis, osteoporosis, osteoarthritis, atherosclerosis, metastasis, wound healing, diabetic retinopathy, ocular vasculopathies, thrombosis, inflammatory bowel disease and other autoimmune diseases.

Also included in the present invention are pharmaceutical kits comprising one or more containers containing pharmaceutical dosage units comprising a compound of Formula I, for the therapeutic inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

DETAILED DESCRIPTION OF THE INVENTION

The present invention provides novel nonpeptide compounds of Formula I (described below) which bind to integrin receptors thereby altering cell-matrix and cell-cell adhesion processes. The compounds of the present invention are useful for the inhibition of cell adhesion and the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis, in a mammal.

One aspect of this invention provides novel compounds of Formula I which are useful as antagonists of the α_(v) β₃ or vitronectin receptor. The compounds of the present invention inhibit the binding of vitronectin and other RGD-containing ligands to α_(v) β₃ and inhibit cell adhesion. The present invention also includes pharmaceutical compositions containing such compounds of Formula I, and methods of using such compounds for the inhibition of angiogenesis, and/or for the treatment of angiogenic disorders.

1! The present invention comprises spirocyclic compounds of Formula I:

    R.sup.1 --Q--W--X--Y                                       (I)

including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein:

Q is selected from ##STR3## A is selected from --N(R¹⁰)--, --(R¹¹)-- or --O--; A¹ is selected from --O-- or --N(R¹⁰)--;

Z is a spiro-fused 4-7 membered ring system (including the sprio atom) containing 0-2 heteroatoms selected from O, S, or N, said ring system optionally being substituted on carbon with keto, or being substituted on carbon or nitrogen independently with 0-2 R⁹ or R¹⁰ or R^(10a) ;

R¹ is selected from: ##STR4## B is independently selected from --CH₂ --, --O--, --N(R²)--, or --C(═O)--;

B¹ is independently selected from --CH₂ -- or --N(R³)--;

D is --N(R²)--, --O--, --S--, --C(═O)-- or --SO₂ --;

E--F is --C(R⁴)═C(R⁵)--, --N═C(R⁴)--, --C(R⁴)═N--, or --C(R⁴)₂ C(R⁵)₂ --;

J, K, L and M are independently selected from --C(R⁴)--, --C(R⁵)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R² is selected from: H, C₁ -C₆ alkyl, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl; (C₁ -C₆ alkyl)aminocarbonyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, heteroaryl(C₁ -C₆ alkyl)carbonyl, heteroarylcarbonyl, aryl C₁ -C₆ alkyl, (C₁ -C₆ alkyl)carbonyl, arylcarbonyl, C₁ -C₆ alkylsulfonyl, arylsulfonyl, aryl(C₁ -C₆ alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C₁ -C₆ alkyl)sulfonyl, aryloxycarbonyl, aryl(C₁ -C₆ alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents independently selected from the group consisting of C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, CF₃, and nitro;

R³ is selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₁ -C₆ alkyl)-;

R⁴ and R⁵ are independently selected from: H, C₁ -C₄ alkoxy, NR² R³, halogen, NO₂, CN, CF₃, C₁ -C₆ alkyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl, arylcarbonyl;

alternatively, when substituents on adjacent atoms, R⁴ and R⁵ can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups independently selected from: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, cyano, amino, CF₃, or NO₂ ;

R⁶ is selected from: H, C₁ -C₄ alkyl, or benzyl;

R⁷ and R⁸ are independently selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₀ -C₆ alkyl)-;

U is selected from:

--N(R⁶) (CH₂)_(n) --,

--N(R⁶) (CH₂)_(m) O--,

--N(R⁶) (CH₂)_(m) N(R⁷)--

--N(R⁶) (CH₂)_(n) S(O)_(p) --

--N(R⁶)C(═O) (CH₂)_(n) --;

--N(R⁶)(CH₂)_(m) C(═O)--;

V is selected from:

--(CH₂)_(n) --,

--(CH₂)_(m) O--(CH₂)_(n) --,

--(CH₂)_(m) N(R⁷) (CH₂)_(n--),

--(CH₂)_(n) S(O)_(p) (CH₂)_(n) --,

--(CH₂)_(m) N(R⁷)C(═O) (CH₂)_(n) --,

--(CH₂)_(n) C(═O)N(R⁷) (CH₂)_(n) --,

--(CH₂)_(n) C(═O) (CH₂)_(n) --;

R⁹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl;

R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl;

W is selected from:

C₁ -C₄ alkylene,

--(C(R¹²)₂)_(q) O(C(R¹²)₂)_(q) --,

--(C(R¹²)₂)_(q) C(═O) (C(R¹²)₂)_(q) --,

--(C(R¹²)₂)_(q) C(═O)N(R¹³)--,

--C(═O)--N(R¹³)--(C(R¹²)₂)_(q) --;

X is --(C(R¹²)₂)_(q) C(R¹²) (R¹⁴)--C(R¹²) (R¹⁵)--;

alternatively, W and X can be taken together to be ##STR5## R¹² is selected from H, C₁ -C₆ alkyl, C₂ -C₆ alkenyl, C₂ -C₆ alkynyl, C₃ -C₇ cycloalkyl, C₄ -C₁₀ cycloalkylalkyl, (C₁ -C₄ alkyl)carbonyl, aryl, or aryl(C₁ -C₆ alkyl)-;

R¹³ is selected from H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkylmethyl, or aryl(C₁ -C₆ alkyl)-

R¹⁴ is selected from:

H, C₁ -C₆ alkylthio(C₁ -C₆ alkyl)-, aryl(C₁ -C₁₀ alkylthioalkyl)-, aryl (C₁ -C₁₀ alkoxyalkyl)-, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₆ hydroxyalkyl, C₂ -C₁₀ alkenyl, C₂ -C₁₀ alkynyl, C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl (C₁ -C₆ alkyl)-, heteroaryl (C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, or CONR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-1 R¹⁶ or 0-2 R¹¹ ;

R¹⁵ is selected from:

H, R¹⁶, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₁₀ alkylaminoalkyl, C₁ -C₁₀ dialkylaminoalkyl, (C₁ -C₁₀ alkyl)carbonyl, aryl(C₀ -C₆ alkyl)carbonyl, C₁ -C₁₀ alkenyl, C₁ -C₁₀ alkynyl , C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl (C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, SO₂ R¹⁷ or SO₂ NR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-2 R¹¹ ;

Y is selected from:

--COR¹⁹, --SO₃ H, --PO₃ H, tetrazolyl, --CONHNHSO₂ CF₃, --CONHSO₂ R¹⁷, --CONHSO₂ NHR¹⁷, --NHCOCF₃, --NHCONHSO₂ R¹⁷, --NHSO₂ R¹⁷, --OPO₃ H₂, --OSO₃ H, --PO₃ H₂, --SO₃ H, --SO₂ NHCOR¹⁷, --SO₂ NHCO₂ R¹⁷, ##STR6## R¹⁶ is selected from: --N(R²⁰)--C(═O)--O--R¹⁷,

--N(R²⁰)--C(═O)--R¹⁷,

--N(R²⁰)--C(═O)--NH--R¹⁷,

--N(R²⁰)SO₂ --R¹⁷, or

--N(R²⁰)SO₂ --NR²⁰ R¹⁷ ;

R¹⁷ is selected from:

C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)heteroaryl, arylaryl(C₁ -C₆ alkyl)-, heteroarylaryl(C₁ -C₆ alkyl)-, arylheteroaryl(C₁ -C₆ alkyl)-, heteroarylheteroaryl (C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ;

R¹⁸ is selected from:

H,

--C(═O)--O--R¹⁷,

--C(═O)--R¹⁷,

--C(═O)--NH--R¹⁷,

--SO₂ --R¹⁷, or

--SO₂ --NR²⁰ R¹⁷ ;

R¹⁹ is selected from:

hydroxy,

C₁ -C₁₀ alkyloxy,

C₃ -C₁₁ cycloalkyloxy,

aryloxy,

aryl(C₁ -C₆ alkoxy)-,

C₃ -C₁₀ alkylcarbonyloxyalkyloxy,

C₃ -C₁₀ alkoxycarbonyloxyalkyloxy,

C₂ -C₁₀ alkoxycarbonylalkyloxy,

C₅ -C₁₀ cycloalkylcarbonyloxyalkyloxy,

C₅ -C₁₀ cycloalkoxycarbonyloxyalkyloxy,

C₅ -C₁₀ cycloalkoxycarbonylalkyloxy,

C₇ -C₁₁ aryloxycarbonylalkyloxy,

C₈ -C₁₂ aryloxycarbonyloxyalkyloxy,

C₈ -C₁₂ arylcarbonyloxyalkyloxy,

C₅ -C₁₀ alkoxyalkylcarbonyloxyalkyloxy,

C₅ -C₁₀ (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy,

C₁₀ -C₁₄ (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or

(R¹¹) (R¹²)N--(C₁ -C₁₀ alkoxy)-;

R²⁰ is selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl (C₁ -C₆ alkyl)-;

m is 1-2;

n is 0-2;

p is 0-2;

q is 0-2; and

r is 0-2;

provided that:

n, q, and r are chosen such that the number of in-chain atoms between R¹ and Y is in the range of 8-18.

2! Preferred compounds of the invention as described above are spirocyclic compounds of Formula I:

    R.sup.1 --Q--W--X--Y                                       (I)

including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein:

Q is selected from ##STR7## R¹ is selected from: ##STR8## D is --N(R²)--, --O--, --S--, --C(═O)-- or --SO₂ --; E--F is --C(R⁴)═C(R⁵)--, --N═C(R⁴)--, --C(R⁴)═N--, or --C(R⁴)₂ C(R⁵)₂ --;

J, K, L and M are independently selected from --C(R⁴)--, --C(R⁵)-- or --N--, provided that at least one of J, K, L and M is not --N--;

R² is selected from: H, C₁ -C₆ alkyl, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl; (C₁ -C₆ alkyl)aminocarbonyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, heteroaryl(C₁ -C₆ alkyl)carbonyl, heteroarylcarbonyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)carbonyl, arylcarbonyl, C₁ -C₆ alkylsulfonyl, arylsulfonyl, aryl(C₁ -C₆ alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C₁ -C₆ alkyl)sulfonyl, aryloxycarbonyl, or aryl (C₁ -C₆ alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents independently selected from the group consisting of C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, CF₃, and nitro;

R³ is selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl (C₁ -C₆ alkyl)-;

R⁴ and R⁵ are independently selected from: H, C₁ -C₄ alkoxy, NR² R³, halogen, NO₂, CN, CF₃, C₁ -C₆ alkyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl, arylcarbonyl, or

alternatively, when substituents on adjacent atoms, R⁴ and R⁵ can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups independently selected from: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, cyano, amino, CF₃, or NO₂ ;

R⁶ is selected from: H, C₁ -C₄ alkyl, or benzyl;

R⁷ and R⁸ are independently selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₀ -C₆ alkyl)-;

U is selected from:

--N(R⁶) (CH₂)_(n) --,

--N(R⁶) (CH₂)_(m) O--,

--N(R⁶) (CH₂)_(m) N(R⁷)--

--N(R⁶) (CH₂)_(n) S(O)p--

--N(R⁶)C(═O) (CH₂)_(n) --;

V is selected from:

--(CH₂)_(n) --,

--(CH₂)_(m) O--(CH₂)_(n) --,

--(CH₂)_(m) N(R⁷) (CH₂)_(n) --,

--(CH₂)_(n) S(O)_(p) (CH₂)_(n) --,

--(CH₂)_(m) N(R⁷)C(═O) (CH₂)_(n) --,

--(CH₂)_(n) C(═O)N(R⁷) (CH₂)_(n) --,

--(CH₂)_(n) C(═O) (CH₂)_(n) --;

R⁹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl;

R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C_(l) -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl;

W is selected from:

C₁ -C₄ alkylene,

--(C(R¹²)₂)_(q) O(C(R¹²)₂)_(q) --,

--(C(R¹²)₂)_(q) C(═O) (C(R¹²)₂)_(q) --,

--(C(R¹²)₂)_(q) C(═O)N(R¹³)--,

--C(═O)--N(R¹³)--(C(R¹²)₂)_(q) --;

X is --(C(R¹²)₂)_(q) C(R¹²) (R¹⁴)--C(R¹²) (R¹⁵)--;

alternatively, W and X can be taken together to be ##STR9## R¹² is selected from H, C₁ -C₆ alkyl, C₂ -C₆ alkenyl, C₂ -C₆ alkynyl, C₃ -C₇ cycloalkyl, C₄ -C₁₀ cycloalkylalkyl, (C₁ -C₄ alkyl)carbonyl, aryl, or aryl(C₁ -C₆ alkyl)-;

R¹³ is selected from H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkylmethyl, or aryl (C₁ -C₆ alkyl)-;

R¹⁴ is selected from:

H, C₁ -C₆ alkylthio(C₁ -C₆ alkyl)-, aryl(C₁ -C₁₀ alkylthioalkyl)-, aryl(C₁ -C₁₀ alkoxyalkyl)-, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₆ hydroxyalkyl, C₂ -C₁₀ alkenyl, C₂ -C₁₀ alkynyl, C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl(C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, or CONR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-1 R¹⁶ or 0-2 R¹¹ ;

R¹⁵ is selected from:

H, R¹⁶, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₁₀ alkylaminoalkyl, C₁ -C₁₀ dialkylaminoalkyl, (C₁ -C₁₀ alkyl)carbonyl, aryl(C₀ -C₆ alkyl)carbonyl, C₁ -C₁₀ alkenyl, C₁ -C₁₀ alkynyl , C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl(C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, SO₂ R¹⁷ or SO₂ NR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-2 R¹¹ ;

Y is selected from:

--COR¹⁹, --SO₃ H, --PO₃ H, tetrazolyl, --CONHNHSO₂ CF₃, --CONHSO₂ R¹⁷, --CONHSO₂ NHR¹⁷, --NHCOCF₃, --NHCONHSO₂ R¹⁷, --NHSO₂ R¹⁷, --OPO₃ H₂, --OSO₃ H, --PO₃ H₂, --SO₃ H, --SO₂ NHCOR¹⁷, --SO₂ NHCO₂ R¹⁷, ##STR10## R¹⁶ is selected from: --N(R²⁰)--C(═O)--O--R¹⁷,

--N(R²⁰)--C(═O)--R¹⁷,

--N(R²⁰)--C(═O)--NH--R¹⁷,

--N(R²⁰)SO₂ --R¹⁷, or

--N(R²⁰) SO₂ --NR²⁰ R¹⁷ ;

R¹⁷ is selected from:

C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)heteroaryl, arylaryl(C₁ -C₆ alkyl)-, heteroarylaryl(C₁ -C₆ alkyl)-, arylheteroaryl(C₁ -C₆ alkyl)-, heteroarylheteroaryl(C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ;

R¹⁸ is selected from:

H,

--C(═O)--O--R¹⁷,

--C(═O)--R¹⁷,

--C(═O)--NH--R¹⁷,

--SO₂ --R¹⁷, or

--SO₂ --NR²⁰ R¹⁷ ;

R¹⁹ is selected from:

hydroxy,

C₁ -C₁₀ alkyloxy,

C₃ -C₁₁ cycloalkyloxy,

aryloxy,

aryl(C₁ -C₆ alkoxy)-,

C₃ -C₁₀ alkylcarbonyloxyalkyloxy,

C₃ -C₁₀ alkoxycarbonyloxyalkyloxy,

C₂ -C₁₀ alkoxycarbonylalkyloxy,

C₅ -C₁₀ cycloalkylcarbonyloxyalkyloxy,

C₅ -C₁₀ cycloalkoxycarbonyloxyalkyloxy,

C₅ -C₁₀ cycloalkoxycarbonylalkyloxy,

C₇ -C₁₁ aryloxycarbonylalkyloxy,

C₈ -C₁₂ aryloxycarbonyloxyalkyloxy,

C₈ -C₁₂ arylcarbonyloxyalkyloxy,

C₅ -C₁₀ alkoxyalkylcarbonyloxyalkyloxy,

C₅ -C₁₀ (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy,

C₁₀ -C₁₄ (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or

(R¹¹) (R¹²)N--(C₁ -C₁₀ alkoxy)-;

R²⁰ selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₁ -C₆ alkyl)-;

m is 1-2;

n is 0-2;

p is 0-2;

q is 0-2; and

r is 0-2;

provided that:

n, q, and r are chosen such that the number of in-chain atoms between R¹ and Y is in the range of 8-18.

3! Further preferred compounds of the invention as described above are compounds of the Formula I including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein:

Q is selected from: ##STR11## R¹ is selected from: ##STR12## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH₂, halogen, NO₂, CN, CF₃, C₁ -C₄ alkoxy, C₁ -C₆ alkyl, and C₃ -C₇ cycloalkyl;

R² is selected from: H, C₁ -C₄ alkyl or benzyl;

U is --NH(CH₂)_(n) --;

V is --(CH₂)_(n) --;

R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C_(1-C) ₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl;

W is --C(═O)--N(R¹³)--;

X is --CH(R¹⁴)--CH(R¹⁵)--;

R¹³ is H or CH₃ ;

R¹⁴ is selected from:

H, C₁ -C₁₀ alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ;

R¹⁵ is H or R¹⁶ ;

Y is --C(═O)R¹⁹ ;

R¹⁶ is selected from:

--N(R²⁰)--C(═O)--O--R¹⁷,

--N(R²⁰)--C(═O)--R¹⁷,

--N(R²⁰)--C(═O)--NH--R¹⁷,

--N(R²⁰)SO₂ --R¹⁷, or

--N(R²⁰)SO₂ --N(R²⁰)R¹⁷ ;

R¹⁷ is selected from:

C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl) heteroaryl, arylaryl(C₁ -C₆ alkyl)-, heteroarylaryl(C₁ -C₆ alkyl)-, arylheteroaryl(C₁ -C₆ alkyl)-, heteroarylheteroaryl(C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ;

R¹⁹ is selected from:

hydroxy,

C₁ -C₁₀ alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

dimethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R²⁰ is H or CH₃ ; and

n is 0-1.

4! Still further preferred compounds of the above invention as described above are compounds of the Formula I including stereoisomeric forms thereof, or mixtures of stereoisomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof wherein:

Q is selected from: ##STR13## R¹ is selected from: ##STR14## R² is selected from: H, C₁ -C₄ alkyl, or benzyl; U is --NH(CH₂)_(n) --;

V is --(CH₂)_(n) --;

R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R^(10a) is selected from : CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ;

R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl;

W is --C(═O)--N(R¹³)--;

X is --CH(R¹⁴)--CH(R¹⁵)--;

R¹³ is H or CH₃ ;

R¹⁴ is selected from:

H, C₁ -C₁₀ alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ;

R¹⁵ is H or R¹⁶ ;

Y is --C(═O)R¹⁹ ;

R¹⁶ is selected from:

--N(R²⁰)--C(═O)--O--R¹⁷ ₁,

--N(R²⁰)--C(═O)--R¹⁷,

--N(R²⁰)SO₂ --R¹⁷,

R¹⁷ is selected from:

C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)heteroaryl, arylaryl(C₁ -C₆ alkyl)-, heteroarylaryl (C₁ -C₆ alkyl)-, arylheteroaryl (C₁ -C₆ alkyl)-, heteroarylheteroaryl(C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ;

R¹⁹ is selected from:

hydroxy,

C₁ -C₁₀ alkoxy,

methylcarbonyloxymethoxy-,

ethylcarbonyloxymethoxy-,

t-butylcarbonyloxymethoxy-,

cyclohexylcarbonyloxymethoxy-,

1-(methylcarbonyloxy)ethoxy-,

1-(ethylcarbonyloxy)ethoxy-,

1-(t-butylcarbonyloxy)ethoxy-,

1-(cyclohexylcarbonyloxy)ethoxy-,

i-propyloxycarbonyloxymethoxy-,

t-butyloxycarbonyloxymethoxy-,

1-(i-propyloxycarbonyloxy)ethoxy-,

1-(cyclohexyloxycarbonyloxy)ethoxy-,

1-(t-butyloxycarbonyloxy)ethoxy-,

dimethylaminoethoxy-,

diethylaminoethoxy-,

(5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-,

(1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or

1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-;

R²⁰ is H or CH₃ ; and

n is 0-1.

5! Specifically preferred compounds of the above invention are compounds including enantiomeric or diasteriomeric forms thereof, or mixtures of enantiomeric or diastereomeric forms thereof, or pharmaceutically acceptable salt or prodrug forms thereof, selected from the group consisting of:

(S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (3,5-dimethylisoxazol4-yl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 8- (6-aminopyridin-2-yl)methyl!-!-1-oxa-2,8-diazaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 8- (6-aminopyridin-2-yl)methyl!!-1-oxa-2,8-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 8- 2-(4,5-dihydroimidazol-2-yl)aminomethyl!-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-methylphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-chloro-4-methylphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (4-biphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-bromophenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (1-naphthyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid.

(S)-2-phenylsulfonylamino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- biphenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- biphenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- biphenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- biphenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- biphenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-phenylsulfonylamino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2-benzyloxycarbonylamino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid,

(S)-2- biphenylsulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, and

(S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-benzimidazolyl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid.

In the present invention it has been discovered that the compounds of Formula I above are useful as inhibitors of cell-matrix and cell-cell adhesion processes. The present invention includes novel compounds of Formula I and methods for using such compounds for the prevention or treatment of diseases resulting from abnormal cell adhesion to the extracellular matrix which comprises administering to a host in need of such treatment a therapeutically effective amount of such compound of Formula I. In the present invention it has also been discovered that the compounds of Formula I above are useful as inhibitors of α_(v) β₃. The compounds of the present invention inhibit the binding of vitronectin to α_(v) β₃ and inhibit cell adhesion.

The present invention also provides pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier.

The compounds of Formula I of the present invention are useful for the treatment (including prevention) of angiogenic disorders. The term "angiogenic disorders" as used herein includes conditions involving abnormal neovascularization, such as tumor metastasis and ocular neovascularization, including, for example, diabetic retinopathy, neovascular glaucoma, age-related macular degeneration, and retinal vein occlusion, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I described above.

The compounds of Formula I of the present invention may be useful for the treatment or prevention of other diseases which involve cell adhesion processes, including, but not limited to, inflammation, bone degradation, thromboembolic disorders, restenosis, rheumatoid arthritis, asthma, allergies, adult respiratory distress syndrome, graft versus host disease, organ transplantation rejection, septic shock, psoriasis, eczema, contact dermatitis, osteoporosis, osteoarthritis, atherosclerosis, inflammatory bowel disease and other autoimmune diseases. The compounds of Formula I of the present invention may also be useful for wound healing.

The term "thromboembolic disorders" as used herein includes conditions involving platelet activation and aggregation, such as arterial or venous cardiovascular or cerebrovascular thromboembolic disorders, including, for example, thrombosis, unstable angina, first or recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary and cerebral arterial thrombosis, myocardial infarction, cerebral embolism, kidney embolisms, pulmonary embolisms, or such disorders associated with diabetes, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I described above.

The compounds of the present invention may be used for other ex vivo applications to prevent cellular adhesion in biological samples. The compounds of the present invention can also be administered in combination with one or more additional therapeutic agents selected from: anti-coagulant or coagulation inhibitory agents, such as heparin or warfarin; anti-platelet or platelet inhibitory agents, such as aspirin, piroxicam, or ticlopidine; thrombin inhibitors such as boropeptides, hirudin or argatroban; or thrombolytic or fibrinolytic agents, such as plasminogen activators, anistreplase, urokinase, or streptokinase.

The compounds of Formula I of the present invention can be administered in combination with one or more of the foregoing additional therapeutic agents, thereby to reduce the doses of each drug required to achieve the desired therapeutic effect. Thus, the combination treatment of the present invention permits the use of lower doses of each component, with reduced adverse, toxic effects of each component. A lower dosage minimizes the potential of side effects of the compounds, thereby providing an increased margin of safety relative to the margin of safety for each component when used as a single agent. Such combination therapies may be employed to achieve synergistic or additive therapeutic effects for the treatment of thromboembolic disorders.

By "therapeutically effective amount" it is meant an amount of a compound of Formula I that when administered alone or in combination with an additional therapeutic agent to a cell or mammal is effective to prevent or ameliorate the thromboembolic disease condition or the progression of the disease.

By "administered in combination" it is meant that the compound of Formula I and one or more additional therapeutic agents are administered concurrently to the mammal being treated. When administered in combination each component may be administered at the same time or sequentially in any order at different points in time. Thus, each component may be administered separately but sufficiently closely in time so as to provide the desired therapeutic effect.

The term anti-coagulant agents (or coagulation inhibitory agents), as used herein, denotes agents that inhibit blood coagulation. Such agents include warfarin (available as COUMADIN®) and heparin. The term anti-platelet agents (or platelet inhibitory agents), as used herein, denotes agents that inhibit platelet function such as by inhibiting the aggregation, adhesion or granular secretion of platelets. Such agents include the various known non-steroidal anti-inflammatory drugs such as aspirin, ibuprofen, naproxen, sulindac, indomethacin, mefenamate, droxicam, diclofenac, sulfinpyrazone, and piroxicam, including pharmaceutically acceptable salts or prodrugs thereof. Other suitable anti-platelet agents include ticlopidine, including pharmaceutically acceptable salts or prodrugs thereof. Ticlopidine is also a preferred compound since it is known to be gentle on the gastro-intestinal tract in use. Still other suitable platelet inhibitory agents include thromboxane-A2-receptor antagonists and thromboxane-A2-synthetase inhibitors, as well as pharmaceutically acceptable salts or prodrugs thereof. The phrase thrombin inhibitors (or anti-thrombin agents), as used herein, denotes inhibitors of the serine protease thrombin. By inhibiting thrombin, various thrombin-mediated processes, such as thrombin-mediated platelet activation (that is, for example, the aggregation of platelets, and/or the granular secretion of plasminogen activator inhibitor-1 and/or serotonin) and/or fibrin formation are disrupted. Such inhibitors include boroarginine derivatives and boropeptides, hirudin and argatroban, including pharmaceutically acceptable salts and prodrugs thereof. Boroarginine derivatives and boropeptides include N-acetyl and peptide derivatives of boronic acid, such as C-terminal α-aminoboronic acid derivatives of lysine, ornithine, arginine, homoarginine and corresponding isothiouronium analogs thereof. The term hirudin, as used herein, includes suitable derivatives or analogs of hirudin, referred to herein as hirulogs, such as disulfatohirudin. Boropeptide thrombin inhibitors include compounds described in Kettner et al., U.S. Pat. No. 5,187,157 and European Patent Application Publication No. 293 881 A2, the disclosures of which are hereby incorporated herein by reference. Other suitable boroarginine derivatives and boropeptide thrombin inhibitors include those disclosed in PCT Application Publication Number 92/07869 and European Patent Application Publication Number 471 651 A2, the disclosures of which are hereby incorporated herein by reference, in their entirety.

The phrase thrombolytics (or fibrinolytic) agents (or thrombolytics or fibrinolytics), as used herein, denotes agents that lyse blood clots (thrombi). Such agents include tissue plasminogen activator, anistreplase, urokinase or streptokinase, including pharmaceutically acceptable salts or prodrugs thereof. Tissue plasminogen activator (tPA) is commercially available from Genentech Inc., South San Francisco, Calif. The term anistreplase, as used herein, refers to anisoylated plasminogen streptokinase activator complex, as described, for example, in European Patent Application No. 028,489, the disclosures of which are hereby incorporated herein by reference herein, in their entirety. The term urokinase, as used herein, is intended to denote both dual and single chain urokinase, the latter also being referred to herein as prourokinase.

Administration of the compounds of Formula I of the invention in combination with such additional therapeutic agent, may afford an efficacy advantage over the compounds and agents alone, and may do so while permitting the use of lower doses of each. A lower dosage minimizes the potential of side effects, thereby providing an increased margin of safety.

The compounds of the present invention are also useful as standard or reference compounds, for example as a quality standard or control, in tests or assays involving the binding of vitronectin or fibrinogen to α_(v) β₃. Such compounds may be provided in a commercial kit, for example, for use in pharmaceutical research involving α_(v) β₃. The compounds of the present invention may also be used in diagnostic assays involving α_(v) β₃.

The compounds herein described may have asymmetric centers. Unless otherwise indicated, all chiral, diastereomeric and racemic forms are included in the present invention. Many geometric isomers of olefins, C═N double bonds, and the like can also be present in the compounds described herein, and all such stable isomers are contemplated in the present invention. It will be appreciated that compounds of the present invention that contain asymmetrically substituted carbon atoms may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis, from optically active starting materials. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomer form is specifically indicated.

When any variable (for example but not limited to, R², R⁴, R⁶, R⁷, R⁸, R¹², and R¹⁴, n etc.) occurs more than one time in any constituent or in any formula, its definition on each occurrence is independent of its definition at every other occurrence. Thus, for example, if a group is shown to be substituted with 0-2 R⁴, then said group may optionally be substituted with up to two R⁴ and R⁴ at each occurrence is selected independently from the defined list of possible R⁴. Also, by way of example, for the group --N(R^(5a))₂, each of the two R^(5a) substituents on N is independently selected from the defined list of possible R^(5a). Similarly, by way of example, for the group --C(R⁷)₂ --, each of the two R⁷ substituents on C is independently selected from the defined list of possible R⁷.

When a bond to a substituent is shown to cross the bond connecting two atoms in a ring, then such substituent may be bonded to any atom on the ring. When a bond joining a substituent to another group is not specifically shown or the atom in such other group to which the bond joins is not specifically shown, then such substituent may form a bond with any atom on such other group.

When a substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of Formula I, then such substituent may be bonded via any atom in such substituent. For example, when the substituent is piperazinyl, piperidinyl, or tetrazolyl, unless specified otherwise, said piperazinyl, piperidinyl, tetrazolyl group may be bonded to the rest of the compound of Formula I via any atom in such piperazinyl, piperidinyl, tetrazolyl group.

Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. By stable compound or stable structure it is meant herein a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.

The term "substituted", as used herein, means that any one or more hydrogen on the designated atom is replaced with a selection from the indicated group, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substituent is keto (i.e., ═O), then 2 hydrogens on the atom are replaced.

As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms (for example, "C₀ -C₁₀ " denotes alkyl having 0 to 10 carbon atoms; thus, C₀ denotes a direct bond between the groups linked by the C₀ group); "haloalkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen (for example --C_(v) F_(w) where v=1 to 3 and w=1 to (2v+1)); "alkoxy" represents an alkyl group of indicated number of carbon atoms attached through an oxygen bridge; "cycloalkyl" is intended to include saturated ring groups, including mono-, bi- or poly-cyclic ring systems, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, and adamantyl; and "biycloalkyl" is intended to include saturated bicyclic ring groups such as 3.3.0!bicyclooctane, 4.3.0!bicyclononane, 4.4.0!bicyclodecane (decalin), 2.2.2!bicyclooctane, and so forth. "Alkenyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more unsaturated carbon-carbon bonds which may occur in any stable point along the chain, such as ethenyl, propenyl and the like; and "alkynyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more triple carbon-carbon bonds which may occur in any stable point along the chain, such as ethynyl, propynyl and the like.

The terms "alkylene", "alkenylene", "phenylene", and the like, refer to alkyl, alkenyl, and phenyl groups, respectively, which are connected by two bonds to the rest of the structure of Formula I. Such "alkylene", "alkenylene", "phenylene", and the like, may alternatively and equivalently be denoted herein as "-(alkyl)-", "-(alkyenyl)-" and "-(phenyl)-", and the like.

"Halo" or "halogen" as used herein refers to fluoro, chloro, bromo and iodo; and "counterion" is used to represent a small, negatively charged species such as chloride, bromide, hydroxide, acetate, sulfate and the like.

As used herein, "aryl" or "aromatic residue" is intended to mean phenyl or naphthyl; the term "arylalkyl" represents an aryl group attached through an alkyl bridge.

As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 7-membered monocyclic or bicyclic or 7- to 14-membered bicyclic or tricyclic or an up to 26-membered polycyclic carbon ring, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocyles include, but are not limited to, cyclopropyl, cyclopentyl, cyclohexyl, phenyl, biphenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl (tetralin).

As used herein, the term "heterocycle" or "heterocyclic" is intended to mean a stable 5- to 7-membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which may be saturated, partially unsaturated, or aromatic, and which consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, O and S and wherein the nitrogen and sulfur heteroatoms may optionally be oxidized, and the nitrogen may optionally be quaternized, and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The heterocyclic rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. Examples of such heterocycles include, but are not limited to, pyridyl (pyridinyl), pyrimidinyl, furanyl (furyl), thiazolyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, tetrazolyl, benzofuranyl, benzothiophenyl, indolyl, indolenyl, isoxazolinyl, isoxazolyl, quinolinyl, isoquinolinyl, benzimidazolyl, piperidinyl, 4-piperidonyl, pyrrolidinyl, 2-pyrrolidonyl, pyrrolinyl, tetrahydrofuranyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, decahydroquinolinyl or octahydroisoquinolinyl, azocinyl, triazinyl, 6H-1,2,5-thiadiazinyl, 2H,6H-1,5,2-dithiazinyl, thianthrenyl, pyranyl, isobenzofuranyl, chromenyl, xanthenyl, phenoxathiinyl, 2H-pyrrolyl, pyrrolyl, imidazolyl, pyrazolyl, isothiazolyl, isoxazolinyl, isoxazolyl, oxazolyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolizinyl, isoindolyl, 3H-indolyl, indolyl, 1H-indazolyl, purinyl, 4H-quinolizinyl, isoquinolinyl, quinolinyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, 4aH-carbazole, carbazole, β-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl, phenazinyl, phenarsazinyl, phenothiazinyl, furazanyl, phenoxazinyl, isochromanyl, chromanyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperidinyl, piperazinyl, indolinyl, isoindolinyl, quinuclidinyl, morpholinyl or oxazolidinyl. Also included are fused ring and spiro compounds containing, for example, the above heterocycles.

As used herein, the term "heteroaryl" refers to aromatic heterocyclic groups. Such heteroaryl groups are preferably 5-6 membered monocyclic groups or 8-10 membered fused bicyclic groups. Examples of such heteroaryl groups include, but are not limited to pyridyl (pyridinyl), pyrimidinyl, furanyl (furyl), thiazolyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, indolyl, isoxazolyl, oxazolyl, pyrazinyl, pyrimidinyl, pyridazinyl, benzofuranyl, benzothienyl, benzimidazolyl, quinolinyl, or isoquinolinyl.

As used herein, "prodrugs" refer to any covalently bonded carriers which release the active parent drug according to Formula I in vivo when such prodrug is administered to a mammalian subject. Prodrugs of the compounds of Formula I are prepared by modifying functional groups present in the compounds in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compounds. Prodrugs include compounds of Formula I wherein hydroxyl, amino, sulfhydryl, or carboxyl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino, sulfhydryl, or carboxyl group respectively. Examples of prodrugs include, but are not limited to, acetate, formate and benzoate derivatives of alcohol and amine functional groups in the compounds of Formula I, and the like.

As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound of Formula I is modified by making acid or base salts of the compound of Formula I. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like.

The pharmaceutically acceptable salts of the compounds of Formula I include the conventional non-toxic salts or the quaternary ammonium salts of the compounds of Formula I formed, for example, from non-toxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like.

The pharmaceutically acceptable salts of the present invention can be synthesized from the compounds of Formula I which contain a basic or acidic moiety by conventional chemical methods. Generally, the salts are prepared by reacting the free base or acid with stoichiometric amounts or with an excess of the desired salt-forming inorganic or organic acid or base in a suitable solvent or various combinations of solvents.

The pharmaceutically acceptable salts of the acids of Formula I with an appropriate amount of a base, such as an alkali or alkaline earth metal hydroxide e.g. sodium, potassium, lithium, calcium, or magnesium, or an organic base such as an amine, e.g., dibenzylethylenediamine, trimethylamine, piperidine, pyrrolidine, benzylamine and the like, or a quaternary ammonium hydroxide such as tetramethylammonium hydroxide and the like.

As discussed above, pharmaceutically acceptable salts of the compounds of the invention can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid, respectively, in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington's Pharmaceutical Sciences, 17th ed., Mack Publishing Company, Easton, Pa., 1985, p. 1418, the disclosure of which is hereby incorporated by reference.

The disclosures of all of the references cited herein are hereby incorporated herein by reference in their entirety.

Synthesis

The compounds of the present invention can be prepared in a number of ways well known to one skilled in the art of organic synthesis. The compounds of the present invention can be synthesized using the methods described below, together with synthetic methods known in the art of synthetic organic chemistry, or variations thereon as appreciated by those skilled in the art. Preferred methods include, but are not limited to, those described below. All references cited herein are hereby incorporated in their entirety herein by reference.

Compounds of Formula I wherein Q includes an isoxazoline ring as one ring of the spirocycle can be conveniently prepared by dipolar cycloaddition of nitrile oxides with appropriate dipolarophiles (for reviews of 1,3-dipolar cycloaddition chemistry, see 1,3-Dipolar Cycloaddition Chemistry (Padwa, ed.), Wiley, New York, 1984; Kanemasa and Tsuge, Heterocycles 1990, 30, 719). The requisite nitrile oxides are in turn prepared from commercially available precursors or appropriately substituted aldehydes via the intermediate oximes.

Scheme 1 illustrates one synthetic sequence which will provide compounds of Formula I of this invention. ##STR15##

Treatment of a methylenecycloalkylmethanol with ethyl chlorooximidoacetate in a suitable solvent, such as tetrahydrofuran or dichloromethane, in the presence of a mild base, such as sodium bicarbonate or triethylamine, provides a spirocycle intermediate, 1(a). Alternately, the cycloaddition can be carried out by thermal decomposition of diethyl nitromalonate in refluxing mesitylene by the method of Shimizu et al. (Bull Chem. Soc. Jpn., 1985, 51, 2519-2522). The hydroxyl group in 1(a) can be subsequently oxidized to the corresponding aldehyde by any of a number of known methods for carrying out this transformation, i.e., (See Manacuso & Swern, Synthesis, 1981, 165; Tidwell, Synthesis, 1990, 857; D. B. Dess & J. C. Martin, J. Org. Chem., 1983, 48, 4155; op cit. J. Amer. Chem. Soc., 1991, 72, 77; R. E. Ireland & L. Liu, J. Org. Chem, 1993, 58, 2899). Reductive amination of the resulting aldehyde with an appropriate aminoheterocycle, such as 2-aminopyridine, can be achieved using sodium triacetoxyborohydride (Abdel-Magid, A. F.; Maryanoff, C. A. Synlett, 1990, 9, 537) to provide a secondary amine. Optional protection of the nitrogen as its BOC derivative yields 1(c). Subsequent hydrolysis of the ethyl ester using conventional methods known to one skilled in the art of organic synthesis gives the corresponding acid 1(d). Coupling of compound 1(d) to an appropriately substituted α- or β-amino ester, 1(e) affords compounds of formula 1(f).

The coupling is carried out using any of the many methods for the formation of amide bonds known to one skilled in the art of organic synthesis. These methods include but are not limited to conversion of the acid to the corresponding acid chloride or fluoride, or use of standard coupling procedures such as the azide method, mixed carbonic acid anhydride (isobutyl chloroformate) method, carbodiimide (dicyclohexylcarbodiimide, diisopropylcarbodiimide, or water-soluble carbodiimides) method, active ester (p-nitrophenyl ester, N-hydroxysuccinic imido ester) method, carbonyldiimidazole method, or coupling with phosphorus reagents such as BOP-Cl. Some of these methods (especially the carbodiimide) can be enhanced by the addition of 1-hydroxybenzotriazole. Deprotection of compound 1(f) is carried out using standard methods of removal of carboxy and amino protecting groups to provide target compounds of formula 1(g).

Additional compounds of formula I can be prepared as shown in Scheme 2. Cycloaddition product, 1(a) can be converted to the corresponding amino compound by conversion to azide 2(a) using diphenylphosphoryl azide under Mitsunobu conditions (Mitsunobu, O. Synthesis 1981, 1) and reduction of the resulting azide with triphenylphosphine (Staudinger, H.; Meyer, J. Helv. Chim. Acta. 1919, 2, 635) Protection of the resulting amino group as its BOC derivative provides intermediate 2(b). Alternately, the amine function can be introduced prior to cycloaddition by conversion of the starting methylenecycloalkylmethanol to the corresponding tosylate, displacement of the tosyl group with sodium azide, reduction to the amine and treatment with di-t-butyldicarbonate. Subsequent 1,3 dipolarcycloaddition provides 2(a). Ester hydrolysis and amide coupling as described above provides compounds of formula 2(d). Hydrolysis of the ester, removal of the BOC protecting group and treatment of the free amine with an appropriate heterocyclic isothiouronium salt, such as those listed in the scheme, provides compounds of Formula 2(f). ##STR16##

Compounds of Formula I, wherein R¹ is a 7-azabenzimidazol-2-yl, group can also be prepared from cycloaddition product 1(a) as depicted in Scheme 3. Jones oxidation of the primary hydroxyl group provides acid 3(a) which is condensed with 2,3-diaminopyridine to provide the 7-azabenzimidazole derivative, 3(b). This intermediate is converted to compounds of the invention by the steps of ester hydrolysis, coupling to compounds of formula 1(e) and deprotection described in detail above. ##STR17##

The appropriately substituted racemic β-amino acids may be purchased commercially or, as is shown in Scheme 4, Method 1, prepared from the appropriate aldehyde, malonic acid and ammonium acetate according to the procedure of Johnson and Livak (J. Am. Chem. Soc. 1936, 58, 299). Racemic β-substituted-β-amino esters may be prepared through the reaction of dialkylcuprates or alkyllithiums with 4-benzoyloxy-2-azetidinone followed by treatment with anhydrous ethanol (Scheme 4, Method 2) or by reductive amination of β-keto esters as is described in WO9316038. (Also see Rico et al., J. Org. Chem. 1993, 58, 7948-51.) Enantiomerically pure β-substituted-β-amino acids can be obtained through the optical resolution of the racemic mixture or can be prepared using numerous methods, including: Arndt-Eistert homologation of the corresponding α-amino acids as shown in Scheme 4, Method 3 (see Meier, and Zeller, Angew. Chem. Int. Ed. Engl. 1975, 14, 32; Rodriguez, et al. Tetrahedron Lett. 1990, 31, 5153; Greenlee, J. Med. Chem. 1985, 28, 434 and references cited within); and through an enantioselective hydrogenation of a dehydroamino acid as is shown in Scheme 4, Method 4 (see Asymmetric Synthesis, Vol. 5, (Morrison, ed.) Academic Press, New York, 1985). A comprehensive treatise on the preparation of β-amino acid derivatives may be found in patent application WO 93/07867, the disclosure of which is hereby incorporated by reference. ##STR18##

The synthesis of N² -substituted diaminopropionic acid derivatives can be carried out via Hoffman rearrangement of a wide variety of asparagine derivatives as described in Synthesis, 266-267, (1981) or by manipulation of the commercially available 3-amino-2-benzyloxycarbonylaminopropionic acid.

Additional dipolarophiles useful for the preparation of the compounds of this invention are either commercially available or may be prepared by numerous methods. Synthesis of representative examples and their conversion into compounds of Formula I are illustrated in the following schemes.

Heating a neat mixture of 8-aza-1,4-dioxaspiro(4,5)decane and 2,6-dibromopyridine provides bromopyridine intermediate 5(a) as shown in Scheme 5. Hydrolysis of the acetal protecting group gives the ketone, 5(b) which can then undergo olefination to compound 5(c). The olefination can be carried out by a number of methods known to one skilled in the art. (For suitable olefination methods, see S. H. Pine et al., Synthesis 1991, 165; Bull. Chem Soc. Jpn., 1980, 53, 1698; or J. Org. Chem. 1968, 33, 780.) The alkene is then subjected to the 1,3-dipolar cycloaddition conditions described above to provide the spirocyclic system, 5(d). Amination with potassium amide in liquid ammonia followed by protection of the resulting amine as its BOC derivative gives compound 5(e). This intermediate is then carried on to compounds of Formula 5(g) using the steps previously described. ##STR19##

Preparation of the analogous (4,4) spiro system is outlined in Scheme 6. Hydrogenation of commercially available 1-benzyl-3-hydroxypyrolidine and selective reprotection of the amine as the t-butylcarbamate provides 6(a). Oxidation of the hydroxyl to the ketone 6(b) by Swern oxidation or other standard methods followed by olefination as described above provides alkene 6(c). This alkene is then subjected to 1,3-dipolar cycloaddition as previously described to provide the spirocycle 6(d). Ester hydrolysis and coupling to a suitable β-amino ester gives 6(e). Removal of the BOC protecting group and treatment with 2-bromo-6-t-butoxycarbonylaminopyridine (Aust. J. Chem. 1982, 35, 2025) gives intermediate 6(f). Finally, deprotection provides compounds of this invention of Formula 6(g). ##STR20##

A further class of spirocycles useful in the present invention is prepared as outlined in Scheme 7. Reduction of N-Cbz 4-hydroxyproline with borane-dimethyl sulfide complex in tetrahydrofuran provides diol 7(a). The primary hydroxyl is then selectively protected as its t-butyldimethylsilyl ether, 7(b). Oxidation of the remaining secondary alcohol using methods described above provides ketone 7(c) which can be converted to alkene 7(d) by olefination. Compound 7(d) then undergoes 1,3-dipolarcycloaddition to provide spirocycle 7(e). Deprotection of the silyl ether by treatment with fluoride ion followed by Swern oxidation of the resulting alcohol provides aldehyde 7(f). Reductive amination with 2-aminopyridine followed by Boc protection of the resulting secondary amine yields 7(g). Ester hydrolysis, coupling to the desired 2,3-diaminopropionate derivative and deprotection gives 7(h). Alternately prior to deprotection the Cbz group can be selectively removed and alternate R¹⁰ groups introduced using standard methods known to one skilled in the art to provide compounds 7(i). ##STR21##

Compounds of Formula I wherein Q includes a 1,2,4-oxadiazoline as one ring of the spriocycle are prepared as shown in Scheme 8. Protection of 4-methylenecyclohexylmethanol as its t-butyldimethylsilyl ether followed by ozonolysis of the double bond provides ketone 8(a). Treatment of compound 8(a) with a suitable amine provides an imine 8(b) which can undergo 1,3-dipolarcycloaddition with a nitrile oxide to provide spirocycle 8(c). Further elaboration as described above would provide additional compounds of the present invention of Formula 8(h). ##STR22##

Additional spirocyclic compounds useful in the present invention can be prepared as outlined in Scheme 9 wherein 1,3-dipolarcycloaddition is carried using ethyl diazoacetate (E. Keller et al., Tetrahedron, 1993, 49, 8899) to provide spirocycle 9(b) (R¹⁰ ═H). The nitrogen of the resulting pyrazole ring may be optionally functionalized using standard methodology prior to carrying out the remaining steps leading to compounds of formula 9(g). ##STR23##

Fully saturated spirocycles are obtained by 1,3-dipolarcycloadditon of α-methoxycarbonylnitrones to an appropriately substituted alkene as illustrated in Scheme 10. (Y. Inouye et al., Bull Chem. Soc. Jpn, 1979, 52, 3763; J. Hara et al., ibid., 1981, 54, 3871). ##STR24##

The detailed processes for preparing the compounds of Formula I are illustrated by the following Examples. It is, however, understood that this invention is not limited to the specific details of these examples. Melting points (mp) are uncorrected. Proton nuclear magnetic resonance spectra (NMR) were measured in chloroform-d (CDCl₃) unless otherwise specified and the peaks are reported in parts per million (ppm) downfield from tetramethylsilane (TMS). The coupling patterns are reported as follows: s, singlet; d, doublet; t, triplet; q, quartet; m, multiplet; bs, broad singlet; bm, broad multiplet. Infrared spectra are reported in reciprocal centimeters (cm⁻¹). All final compounds gave satisfactory nmr and HRMS data and were analyzed to be >98% pure by reverse phase analytical HPLC.

EXAMPLES Example 1081 (S)-2-benzyloxycarbonylamino-3- 8-(2-pyridinylamino)methyl-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid Ethyl (8-hydroxymethyl)-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carboxylate: 1(a)

Method A

4-Methylenecyclohexylmethanol (2.52 g, 20 mmol, Wiley Organics, 63% purity) and sodium bicarbonate (8.4 g, 100 mmol) in 45 ml of 2:1 THF:H₂ O was cooled in an ice bath. Ethyl chlorooximidoacetate (5.00 g, 33 mmol) in 30 ml 2:1 THF:H₂ O was then added, and the mixture stirred at room temperature for 18 hours. The mixture was then diluted with ethyl acetate and washed with water. The aqueous layer was extracted with one more portion of ethyl acetate. The organic layers were combined, dried (MgSO₄), filtered, concentrated and the residue purified by flash chromatography (silica gel column/1:1 EtOAc:Hexane) to afford 1(a) as a colorless oil (57.6% yield). HRMS calcd. for C₁₂ H₁₉ NO₄ ( M+H!⁺): 242.139233; found: 242.140376.

Method B

A mixture of 4-Methylenecyclohexylmethanol (10 g, mol, Wiley Organics, 63% purity, 0.051 mol) and diethylnitromalonate (14 ml, 0.08 mol) in 100 ml mesitylene was refluxed for 4-5 hrs under a nitrogen atmosphere with stirring. The resulting yellow solution was evaporated on a rotary evaporator in vacuo and the residue purified by flash chromatography (silica gel/70:30 Hexane/ethyl acetate) to provide 6.4 g of 1(a) (52%) as 3/2 mixture of diastereomers by nmr.

Ethyl (8-formyl)-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carboxylate: 1(b)

Oxalyl chloride (0.70 ml, 8 mmol) in 5 ml CH₂ Cl₂ was cooled to -78° C. in dry ice-acetone bath and treated with dimethylsulfoxide (0.74 ml, 10.4 mmol) in 10 ml CH₂ Cl₂ and stirred at -78° C. for 15 minutes. Intermediate 1(a) (992 mg, 4 mmol) in 10 ml CH₂ Cl₂ was then added, and the mixture stirred at -78° C. for 1 hour. Triethylamine (2.0 g, 20 mmol) in 5 ml CH₂ Cl₂ was then added, and the mixture stirred at -78° C. for 15 minutes. The bath was removed and the mixture allowed to warm up over a 30 minute period, diluted with CH₂ Cl₂ (50 ml) and washed with water followed by brine. The organic layer was separated, dried over anhydrous magnesium sulfate, filtered and concentrated to afford 0.68 g of 1(b) as a clear oil. HRMS calcd. for C₁₂ H₁₇ NO₄ ( M+H!⁺): 240.123583; found: 240.123665.

Ethyl 8- (N-t-butoxycarbonyl)-(N-2-pyridinyl)aminomethyl!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carboxylate 1(c):

The intermediate 1(b) (1.068 g, 4 mmol crude) and acetic acid (240 mg, 4 mmol) in 15 ml 1,2-dichloroethane were treated with sodium triacetoxyborohydride (1.19 g, 5.6 mmol), and the mixture stirred at room temperature for 18 hours. The mixture was diluted with ethyl acetate and washed with sat. sodium bicarbonate and then brine. The organic layer was separated, dried over anhydrous magnesium sulfate, filtered and concentrated to afford 1.32 g of amine as an oil. HRMS calcd. for C₁₇ H₂₃ N₃ O₃ ( M+H!⁺): 318.181767; found: 318.183254. The crude amine and triethylamine (1.0 g, 10 mmol) in 20 ml dichloromethane were treated with di-t-butyldicarbonate (2.18 g, 10 mmol), and stirred at room temperature for 18 hours. The mixture was diluted with dichloromethane and washed with water and brine. The organic layer was separated, dried over anhydrous magnesium sulfate, filtered, concentrated and the residue purified by flash chromatography (silica gel/1:3 EtOAc:Hexane) to afford 845 mg of 1(c) as a colorless oil (50.6% yield from 1(a)). HRMS calcd. for C₂₂ H₃₁ N₃ O₅ ( M+H!⁺): 418.234197; found: 418.233666.

8- (N-t-Butoxycarbonyl)-(N-2-pyridinyl)aminomethyl!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carboxylic acid 1(d)

The intermediate 1(c) (209 mg, 0.5 mmol) in 4.5 ml of 2:1 THF:H₂ O was treated with lithium hydroxide monohydrate (25 mg, 0.6 mmol) and the mixture stirred at room temperature for 18 hours. The mixture was quenched with 0.6 ml of 1N HCl and extracted with ethyl acetate (2×25 ml). The organic layer was separated, dried over anhydrous magnesium sulfate, filtered, concentrated to afford 199 mg of 1(d) as a colorless foam. HRMS calcd. for C20H27N3O5 ( M+H!⁺): 390.202896; found: 390.202306.

Methyl (S)-2-benzyloxycarbonylamino-3- 8- N-(t-butoxycarbonyl)-N-(2-pyridinyl)amino!methyl-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionate

1(f) (R¹⁵ ═NHCbz, R═Me): The intermediate 1(d) (199 mg, 0.5 mmol crude), 1(e) (R¹⁵ ═NHCbz, R═Me, 144 mg, 0.5 mmol) and BOP Reagent (265 mg, 0.6 mmol) in 3 ml DMF were treated with 4-N-methylmorpholine (152 mg, 1.5 mmol) in 2 ml DMF and the mixture stirred at room temperature for 18 hours. The mixture was diluted with ethyl acetate and washed with sat. sodium bicarbonate, water and then brine. The organic layer was separated, dried over anhydrous magnesium sulfate, filtered, concentrated and the residue purified by flash chromatography (silica gel column/1:1 EtOAc:Hexane followed by 10:1:10 EtOAc:EtOH:Hexane) to afford 213 mg of 1(f) (R¹⁵ ═NHCbz, R═Me) as a white solid (68.3% yield from 1(c)). HRMS calcd. for C₃₂ H₄₁ N₅ O₈ ( M+H!⁺): 624.303339; found: 624.303031.

(S)-2-benzyloxycarbonylamino-3- 8-(2-pyridinylamino)methyl-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid

1(g) (R¹⁵ ↑NHCbz): The intermediate 1(f) (205 mg, 0.33 mmol crude) in 4 ml of 1:1 MeOH:H₂ O was treated with lithium hydroxide monohydrate (21 mg, 0.5 mmol) and the mixture stirred at room temperature for 18 hours. The mixture was neutralised with 0.5 ml of 1N HCl and extracted with EtOAc. The organic layer was separated, dried over anhydrous magnesium sulfate, filtered, concentrated to afford 205 mg of the free acid as a white solid. HRMS calcd. for C₃₁ H₃₉ N₅ O₈ ( M+H!⁺): 610.287689; found: 610.290115. Crude acid was treated with 3 ml of 4M HCl in dioxane and stirred at room temperature for 18 hours. The mixture was concentrated in vacuo and the residue purified by preparative HPLC (C18/80% CH₃ CN:20% H₂ O:0.05% TFA) to afford 132 mg of a white solid. The compound was lyophilyzed from 2 ml of 1:1 CH₃ CN:H₂ O to afford 107 mg of 1(g) (R¹⁵ ═NHCbz) as a white solid (52.0% yield from 1(f)). ¹ H NMR (DMSO-D6; Mixture of diastereoisomers) d 7.8 (m, 2H), 7.35 (bs, 5H), 6.8 (m, 2H), 5.11 (s, 2H), 4.44 (s, 1H), 3.4 (bm, 2H), 3.2 (m, 2H), 2.8 (s, 2H),2.0-1.2 (bm, 8H); HRMS calcd. for C₂₆ H₃₁ N₅ O₆ ( M+H!⁺): 510.235259; found: 510.236039.

Similarly prepared from 1(d) were the following:

Example 1111 (S)-2-phenylsulfonylamino-3- 8-(2-pyridinylamino)methyl-1-oxa-2-azaspiro-4,5!-dec-2-en-3-yl!carbonylamino!propionic acid

¹ H NMR (DMSO-D6) d 8.8 (bs,1H), 8.23 (t, 1H, J=6), 8.18 (d, 1H, J=9), 7.85-7.40 (m, 5H), 7.03 (d, 1H, J=9), 6.8 (t, 1H, J=7), 3.93 (dd, 1H, J=13, 7), 3.38 (m, 1H), 3.19 (bm, 3H), 2.8 (s, 2H), 1.85-1.2 (bm, 8H); MS calcd. for C₂₄ H₂₉ N₅ O₆ S ( M+H!⁺): 516.2; found: 516.1.

Example 1121 (S)-2- (2.5-dimethylisoxazol-2-yl)sulfonyl!amino-3- 8-(2-pyridinylamino)methyl-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid

¹ H NMR (DMSO-D6) d 8.8 (bs,1H), 8.54 (d, 1H, J=9), 8.27 (t, 1H, J=6), 7.86 (m, 1H), 7.03 (d, 1H, J=9), 3.94 (m, 1H), 3.44 (m, 1H), 3.19 (bm, 3H), 2.8 (s, 2H), 2.45 (s, 3H), 2.5 (s, 3H), 2.9-1.2 (bm, 8H); MS calcd. for C₂₃ H₃₀ N₆ O₇ S ( M+H!⁺): 535.2; found: 535.1.

Example 3055 (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylamino)methyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid

Part A: N-Cbz-4-hydroxy-L-prolinol

A solution of N-Cbz-4-hydroxy-L-proline (50 gm, 0.188 mol) in tetrahydrofuran (400 ml) was cooled to 0° C. in an ice bath under nitrogen and a solution of borane dimethylsulfide complex (2.0M in THF, 122 ml, 0.244 mol) was added dropwise over 1 h. The resulting mixture is then allowed to stir overnight at room temperature. the reaction mixture was recooled to 0° C. and a second portion of borane-dimethylsulfide complex was added as described above. Reaction was again stirred at room temperature overnight, then cooled to 0° C. and quenched by addition of approximately 200 ml of 1:1 methanol/water. Solvents were removed on rotary evaporator and residue diluted with water and extracted 4× with ethyl acetate. The combined extracts were washed with saturated aqueous sodium bicarbonate solution (2×) and brine (1×) then dried over anhydrous magnesium sulfate, filtered and evaporated to a clear oil (46.77 g, 99%) which was used without purification in part B below.

Part B. 1-benzyloxycarbonyl-2-(S)-t-butyldimethylsilyloxymethyl-4-hydroxypyrrolidine

A mixture of the compound of Part A above (46.77 g, 0.186 mol), triethylamine (51.8 g, 0.372 mol), and t-butyldimethylsilylchloride (30.86 g, 0.205 mol) in methylene chloride (375 ml) was stirred under nitrogen overnight at room temperature. An additional aliquot of silyl chloride (5 g, 0.033 mol) was added and stirring continued for 4-5 h. Reaction mixture was transferred to a separatory funnel and washed with water (4×) and brine (1×) then dried over anhydrous sodium sulfate, filtered and solvent removed in vacuo. The residue was chromatographed on silica gel (hexane-hexane/ethyl acetate 8:2-hexane/ethyl acetate 7:3) to provide the silyl ether (47.11 g, 69%)

Part C. 1-benzyloxycarbonyl-2(S)-t-butyldimethylsilyloxymethyl-4-pyrrolidinone

To a solution of oxalyl chloride (12.4 ml, 0.142 mol) in methylene chloride (330 ml) precooled to -70° C. in an acetone/dry ice bath was added a solution of anhydrous dimethylsulfoxide (20.60 ml, 0.29 mol) in methylene chloride (66 ml) dropwise under nitrogen over 30 min at T<-65° C. The resulting mixture was stirred 15 min, followed by dropwise addition of a solution of the compound of part B above in methylene chloride (130 ml) over 45 min at T<-65° C. The reaction was stirred for 30 min followed by dropwise addition of triethylamine (119.2 ml, 0.855 mol) over 30 min again at T<-65° C. The cooling bath was removed and the reaction temperature was allowed to rise to 5°-10° C., and then quenched by addition of 645 ml of 10% aqueous potassium hydrogen sulfate solution. The mixture was then transferred to a separatory funnel and layers separated. The aqueous was extracted with methylene chloride and the combined organic layers are washed with 10% citric acid solution (3×) and brine (1×) then dried over anhydrous sodium sulfate, filtered and concentrated to a clear oil (46.8 g, 100%) which was used without purification in part D below.

Part D. 1-benzyloxycarbonyl-2(S)-t-butyldimethylsilyloxymethyl-4-methylenepyrrolidine

Methyltriphenylphosphonium bromide (68,98 g, 0.193 mol) is added to a suspension of potassium t-butoxide (20.27 g, 0.181 mol) in anhydrous ether (700 ml) with stirring at 0° C. under nitrogen. The resulting bright yellow solution is stirred for an additional 15 min. To this is added a solution of the compound of part D above (46.8 g, 0.129 mol) in ether (100 ml). The mixture is allowed to assume room temperature and stirred overnight. The resulting mixture was cooled in an ice bath and quenched by addition 700 ml of a saturated solution of ammonium chloride. The phases were separated and aqueous reextracted 2× with ether. The combined organics were washed with brine and dried over anhydrous sodium sulfate, filtered and evaporated in vacuo. The crude product was purified by flash chromatography (silica gel, hexane-ether 9:1) to provide the olefin (42.6 g, 91%) as a pale yellow oil.

Part E: 7-benzyloxycarbonyl-8-t-butyldimethylsilyloxy-methyl-3-ethoxycarbonyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-ene

The compound of part D above (13.04 g, 0.036 mol) was dissolved in methylene chloride (50 ml), treated with ethyl chlorooximidoacetate (8.18 g., 0.054 mol), and the mixture was cooled to 0° C. followed by dropwise addition of triethylamine (7.53 ml, 0.054 mol). The reaction was allowed to come to room temperature over several hours then stirred overnight. An additional 1.5 eq. of the chlorooxime was then added, and the mixture was cooled to 0° C. and treated with triethylamine (1.5 eq) as described above. Resulting mixture was stirred at room temperature for 48 h, then diluted with additional methylene chloride and washed with 10% aqueous citric acid (3×), and brine (1×) then dried over anhydrous sodium sulfate, filtered and evaporated in vacuo. The crude was charged to silica gel and eluted first with Hexane/ether(80:20) to provide unreacted starting material (6.64 g, 51%) and then with hexane/ethyl acetate (75:25) to provide the two diastereomers of the product (S,S isomer, 5.54 g, 32%; S,R isomer, 1.34 g, 8%). Anal. Calcd. for C₂₄ H₃₆ N₂ O₆ Si: C, 60.48; H, 7.61; N, 5.89. Found: C, 60.46; H, 7.33; N, 5.96.

Part F: 7-benzyloxycarbonyl-8-t-butyldimethylsilyloxy-methyl-3-carboxy-1-oxa-2,7-diazaspiro- 4,4!-non-2-ene

The compound of Part E above (18.7 g, 0.038 mol) was dissolved in methanol (200 ml) and treated at room temperature with a solution of lithium hydroxide monohydrate (2.4 g, 0.057 mol) in water (50 ml). The whole was stirred for 5 h and then solvent removed in vacuo. Water was added and the pH of the solution was adjusted to 4.4 with 10% aq. citric acid solution. The resulting mixture was extracted 3× with ethyl acetate with adjustment of pH back to 4.4 between extractions. The combined extracts were washed with brine and dried over anhydrous sodium sulfate, filtered and evaporated. The residue was dried under vacuum to provide the acid (16.2 g, 95%) as a foam which was used without purification in Part G below. MS(esi) m/z 449.4 (M+H)⁺, 335.2 (M+H-TBMDS)⁺

Part G: t-Butyl (S)-2- (2.4.6-trimethylphenyl)sulfonyl!-amino-3- 7-benzyloxycarbonyl-8-(t-butyldimethylsilyl-oxy)methyl-1-oxa-2.7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid

A mixture of the compound of Part F above (10 g, 0.022 mol), t-butyl 3-amino-2-(2,4,6-trimethylphenylsulfonylamino)propionate (7.6 g, 0.022 mol), N-methylmorpholine (5.4 ml, (0.049 mol) and Castro's reagent (14.8 g, 0.033 mol) in N,N-dimethylformamide (100 ml) was stirred under nitrogen at room temperature overnight. The DMF was removed in vacuo and the residue diluted with 500 ml water and extracted 3× with ethyl acetate. The combined extracts were washed with water (2×), 10% citric acid (1×), saturated sodium bicarbonate (1X) and brine (1X) then dried over anhydrous sodium sulfate, filtered and evaporated. The coupling product was purified by filtration through a pad of silica gel eluted with hexane/ethyl acetate (4:1) to provide the product as a white foam (15 gm, 88%). MS(esi) m/z 773.4 (M+H)⁺ 795.4 (M+Na)⁺.

Part H: t-Butyl (S)-2- (2,4,6-trimethylphenyl)sulfonyl!-amino-3- 7-benzyloxycarbonyl-8-hydroxymethyl-1-oxa-2.7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid

The compound of Part G above (2.8 g, 3.62 mmol) was dissolved in tetrahydrofuran (12 ml) and treated with tetra-n-butylammonium floride (5.8 ml of a 1.0M solution in THF, 5.8 mmol). The resulting solution was stirred overnight at room temperature. Reaction was quenched by addition of water and THF removed on rotary evaporator. The remaining aqueous was extracted 3× with ethyl acetate. The combined extracts were washed with water and brine, dried over anhydrous sodium sulfate, filtered and evaporated. Chromatography on silica gel (hexane/ethyl acetate 1:1 followed by methylene chloride/methanol 95:5) provided the alcohol (2.02 g., 85%) ms m/z 659.3 (M+H)⁺.

Part I: t-Butyl (S)-2- (2,4,6-trimethylphenyl)sulfonyl!-amino-3- 7-benzyloxycarbonyl-8-formyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid

A solution of the compound of Part H above (0.8 g, 1.21 mmol) in anhydrous methylene chloride (1 ml) was added dropwise to a a solution of Dess-Martin periodinane (0.59 g, 1.30 mmol) in approximately 4 ml of dry methylene chloride at room temperature under nitrogen. The resulting mixture was stirred for 1 hr, the diluted with ethyl acetate and poured into a solution of saturated sodium bicarbonate (20 ml) containing 5 g sodium thiosulfate. This was stirred for 10 min. The phases were separated, aqueous reextracted with ethyl acetate, and combined organics washed with saturated sodium bicarbonate, water and brine, then dried over anhydrous magnesium sulfate, filtered and evaporated to give the aldehyde as a clear oil (0.74 g, 93%).

Part J: t-Butyl (S)-2- (2,4,6-trimethylphenyl)sulfonyl!-amino-3- 7-benzyloxycarbonyl-8-(imidazol-2-ylamino)methyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid

To a solution of the compound of Part I above (0.73 g, 1.11 mmol) in benzene was added anhydrous magnesium sulfate (0.588 g, 4.88 mmol) and 2-amino-1-tritylimidazole (0.398 g, 1.22 mmol) and the whole was refluxed for 4 hrs under nitrogen. The mixture was cooled to room temperature, filtered under nitrogen and benzene removed in vacuo. The residue was taken up in 1,2-dichloroethane, treated under nitrogen at room temperature with sodium triacetoxyborohydride (0.588 g, 2.78 mmol), and the whole was stirred overnight. The reaction was quenched by addition of water and then diluted with ethyl acetate. Aqueous was reextracted with ethyl acetate, and combined organic layers were washed with saturated sodium bicarbonate, water and brine, then dried over anhydrous magnesium sulfate, filtered and evaporated. Filtration through silica gel provided the desired product (0.682 g, 63%) as an off-white foam which was used without further purification in part K below.

Part K: (S)-2- (2,4,6-trimethylphenyl)sulfonyl!-amino-3- 7-benzyloxycarbonyl-8-(imidazol-2-ylamino)methyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid

The compound of part J above (0.3 g, 0.31 mmol) was dissolved in 20% acetic acid in methanol (10 ml) and refluxed for 24 h under nitrogen. The reaction was cooled to room temperature, methanol removed by evaporation and residue diluted with ethyl acetate. This solution was washed with saturated sodium bicarbonate (2×), water and brine then dried over anhydrous magnesium sulfate, filtered and evaporated. Filtration through silica gel (eluted with (i)methylene chloride/methanol 95:5; (2) methylene chloride/methanol/conc. ammonium hydroxide 95:5:0/5; (3) 90/10/1) provided the intermediate detritylated t-butyl ester 0.139 mg, 62%). This was taken up in methylene chloride (8 ml) and trifluoroacetic acid (2 ml) was added. The solution was stirred for 72 h, then evaporated and triturated with ether. The resulting solid was purified by prep HPLC (C18, gradient from 100% A to 100% B: A=90/10/0.05 H₂ O/CH₃ CN/TFA; B=90/10/0.05 CH₃ CN/H₂ O/TFA) to provide the title compound (0.078 g, 50%). MS m/z 690.4 (M+Na)⁺ 668.4 (M+H)⁺.

Example 3063 (S)-2- (2,4,6-trimethylphenyl)sulfonyl!-amino-3- 8-(imidazol-2-ylamino)methyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!-propionic acid

The compound of Example 3055, Part J, (0.1 g, 0.1 mmol) was taken up in neat trifluoroacetic acid (3 ml) and the mixture refluxed for 1.5 h. Reaction was cooled to room temperature and TFA removed in vacuo. The residue was purified by prep HPLC using the system described under Ex. 3055, Part K above to provide the title compound (0.043 g, 80%). MS m/z 534.4 (M+H)⁺.

Using the methods described above and modifications thereof known to one skilled in the art of organic synthesis, additional compounds of the present invention can be prepared, including, but not limited to the representative compounds listed in the Tables below.

Utility

The compounds of Formula I of the present invention possess activity as antagonists of integrins such as, for example, the α_(v) β₃ or vitronectin receptor, α_(v) β₅ or α₅ β1, and as such have utility in the treatment and diagnosis of cell adhesion, angiogenic disorders, inflammation, bone degradation, cancer metastases, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis. The integrin antagonist activity of the compounds of the present invention is demonstrated using assays which measure the binding of a specific integrin to a native ligand, for example, using the ELISA assay described below for the binding of vitronectin to the α_(v) β₃ receptor.

The compounds of the present invention possess selectivity for the α_(v) β₃ receptor relative to the GPIIb/IIIa receptor as demonstrated by their lack of activity in standard assays of platelet aggregation, such as the platelet aggregation assay described below.

One of the major roles of integrins in vivo is to mediate cellular interactions with adjacent cells. Cell based adhesion assays can be used to mimic these interactions in vitro. A cell based assay is more representative of the in vivo situation than an ELISA since the receptor is maintained in membranes in the native state. The compounds of the present invention have activity in cell-based assays of adhesion, for example as demonstrated in using the cell adhesion assays described below.

The compounds of Formula I of the present invention may be useful for the treatment or prevention of other diseases which involve cell adhesion processes, including, but not limited to, osteoporosis, rheumatoid arthritis, autoimmune disorders, bone degradation, rheumatoid arthritis, asthma, allergies, adult respiratory distress syndrome, graft versus host disease, organ transplantation, septic shock, psoriasis, eczema, contact dermatitis, osteoarthritis, atherosclerosis, metastasis, wound healing, inflammatory bowel disease and other angiogenic disorders.

The compounds of Formula I have the ability to suppress/inhibit angiogenesis in vivo, for example, as demonstrated using animal models of ocular neovascularization.

The compounds provided by this invention are also useful as standards and reagents in determining the ability of a potential pharmaceutical to inhibit integrin-ligand binding. These may be provided in a commercial kit comprising a compound of this invention.

As used herein "μg" denotes microgram, "mg" denotes milligram, "g" denotes gram, "μL" denotes microliter, "mL" denotes milliliter, "L" denotes liter, "nM" denotes nanomolar, "μM" denotes micromolar, "mM" denotes millimolar, "M" denotes molar and "nm" denotes nanometer. "Sigma" stands for the Sigma-Aldrich Corp. of St. Louis, Mo.

The utility of the compounds of the present invention may be assessed by testing in one or more of the following assays as described in detail below: Purified α_(v) β₃ (human placenta)--Vitronectin ELISA, α_(v) β₃ -Vitronectin Binding Assay, Human Aortic Smooth Muscle Cell Migration Assay, In Vivo Angiogenesis Model, Pig Restenosis Model, Mouse Retinopathy Model. A compound of the present invention is considered to be active if it has an IC₅₀ or K_(i) value of less than about 10 μM for the inhibition of α_(v) β₃ -Vitronectin Binding Assay, with compounds preferably having K_(i) values of less than about 0.1 μM. Tested compounds of the present invention are active in the α_(v) β₃ -Vitronectin Binding Assay as well as in cell-based assays of integrin adhesion mediated by the α_(v) β₃ -receptor.

Purified α_(v) β₃ (human placenta)--Vitronectin ELISA

The α_(v) β₃ receptor was isolated from human placental extracts prepared using octylglucoside. The extracts were passed over an affinity column composed of anti-α_(v) β₃ monoclonal antibody (LM609) to Affigel. The column was subsequently washed extensively at pH 7 and pH 4.5 followed by elution at pH 3. The resulting sample was concentrated by wheat germ agglutinin chromatography to provide gave two bands on SDS gel which were confirmed as α_(v) β₃ by western blotting.

Affinity purified protein was diluted at different levels and plated to 96 well plates. ELISA was performed using fixed concentration of biotinylated vitronectin (approximately 80 nM/well). This receptor preparation contains the α_(v) β₃ with no detectable levels of α_(v) β₅ according to the gel (α_(v) β₃) and according to effects of blocking antibodies for the α_(v) β₃ or α_(v) β₅ in the ELISA.

A submaximal concentration of biotinylated vitronectin was selected based on conc. response curve with fixed receptor conc. and variable concentrations of biotinylated vitronectin.

α_(v) β₃ -Vitronectin Binding Assay

The purified receptor is diluted with coating buffer (20 mM Tris HCl, 150 mM NaCl, 2.0 mM CaCl₂, 1.0 MM MgCl₂.6H₂ O, 1.0 mM MnCl₂.4H₂ O) and coated (100 μL/well) on Costar (3590) high capacity binding plates overnight at 4° C. The coating solution is discarded and the plates washed once with blocking/binding buffer (B/B buffer, 50 mM Tris HCl, 100 mM NaCl, 2.0 mM CaCl₂,1.0 mM MgCl₂.6H₂ O,1.0 mM MnCl₂.4H₂ O). Receptor is then blocked (200 μL/well) with 3.5% BSA in B/B buffer for 2 hours at room temperature. After washing once with 1.0% BSA in B/B buffer, biotinylated vitronectin (100 μL) and either inhibitor (11 μL) or B/B buffer w/1.0% BSA (11 μL)is added to each well. The plates are incubated 2 hours at room temperature. The plates are washed twice with B/B buffer and incubated 1 hour at room temperature with anti-biotin alkaline phosphatase (100 μL/well) in B/B buffer containing 1.0% BSA. The plates are washed twice with B/B buffer and alkaline phosphatase substrate (100 μL) is added. Color is developed at room temperature. Color development is stopped by addition of 2N NaOH (25 μL/well) and absorbance is read at 405 nm. The IC₅₀ is the concentration of test substance needed to block 50% of the vitronectin binding to the receptor.

Integrin Cell-Based Adhesion Assays

In the adhesion assays, a 96 well plate was coated with the ligand (i.e., fibrinogen) and incubated overnight at 4° C. The following day, the cells were harvested, washed and loaded with a fluorescent dye. Compounds and cells were added together and then were immediately added to the coated plate. After incubation, loose cells are removed from the plate, and the plate (with adherent cells) is counted on a fluorometer. The ability of test compounds to inhibit cell adhesion by 50% is given by the IC₅₀ value and represents a measure of potency of inhibition of integrin mediated binding. Compounds were tested for their ability to block cell adhesion using assays specific for α_(v) β₃, α_(v) β₅ and α₅ β₁ integrin interactions.

Platelet Aggregation Assay

Venous blood was obtained from anesthetized mongrel dogs or from healthy human donors who were drug- and aspirin-free for at least two weeks prior to blood collection. Blood was collected into citrated Vacutainer tubes. The blood was centrifuged for 15 minutes at 150×g (850 RPM in a Sorvall RT6000 Tabletop Centrifuge with H-1000 B rotor) at room temperature, and platelet-rich plasma (PRP) was removed. The remaining blood was centrifuged for 15 minutes at 1500×g (26,780 RPM) at room temperature, and platelet-poor plasma (PPP) was removed. Samples were assayed on a PAP-4 Platelet Aggregation Profiler, using PPP as the blank (100% transmittance). 200 μL of PRP (5×10⁸ platelets/mL) were added to each micro test tube, and transmittance was set to 0%. 20 μL of ADP (10 μM) was added to each tube, and the aggregation profiles were plotted (% transmittance versus time). Test agent (20 μL) was added at different concentrations prior to the addition of the platelet agonist. Results are expressed as % inhibition of agonist-induced platelet aggregation.

Human Aortic Smooth Muscle Cell Migration Assay

A method for assessing α_(v) β₃ -mediated smooth muscle cell migration and agents which inhibit α_(v) β₃ -mediated smooth muscle cell migration is described in Liaw et al., J. Clin. Invest. (1995) 95:713-724).

In Vivo Angiogenesis Model

A quantitative method for assessing angiogenesis and antiangiogenic agents is described in Passaniti et al., Laboratory Investigation (1992) 67:519-528

Pig Restenosis Model

A method for assessing restenosis and agents which inhibit restenosis is described in Schwartz et al., J. Am. College of Cardiology (1992) 19:267-274.

Mouse Retinopathy Model

A method for assessing retinopathy and agents which inhibit retinopathy is described in Smith et al., Invest. Ophthal. & Visual Science (1994) 35:101-111.

Dosage and Formulation

The compounds of this invention can be administered by any means that produces contact of the active agent with the agent's site of action, the α_(v) β₃ integrin, in the body of a mammal. They can be administered by any conventional means available for use in conjunction with pharmaceuticals, either as individual therapeutic agents or in a combination of therapeutic agents, such as a antiplatelet agent such as aspirin, piroxicam, or ticlopidine which are agonist-specific, or an anti-coagulant such as warfarin or heparin, or a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof. The compounds of the invention, or compounds of the invention in combination with other therapeutic agents, can be administered alone, but generally administered with a pharmaceutical carrier selected on the basis of the chosen route of administration and standard pharmaceutical practice.

The dosage of the novel cyclic compounds of this invention administered will, of course, vary depending upon known factors, such as the pharmacodynamic characteristics of the particular agent and its mode and route of administration; the age, health and weight of the recipient; the nature and extent of the symptoms; the kind of concurrent treatment; the frequency of treatment; and the effect desired. A daily dosage of active ingredient can be expected to be about 0.001 to 10 milligrams per kilogram of body weight.

Dosage forms (compositions suitable for administration) contain from about 0.1 milligram to about 100 milligrams of active ingredient per unit. In these pharmaceutical compositions the active ingredient will ordinarily be present in an amount of about 0.5-95% by weight based on the total weight of the composition.

The active ingredient can be administered orally in solid dosage forms, such as capsules, tablets, and powders, or in liquid dosage forms, such as elixirs, syrups, and suspensions. It can also be administered parenterally, in sterile liquid dosage forms.

Gelatin capsules contain the active ingredient and powdered carriers, such as lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, and the like. Similar diluents can be used to make compressed tablets. Both tablets and capsules can be manufactured as sustained release products to provide for continuous release of medication over a period of hours. Compressed tablets can be sugar coated or film coated to mask any unpleasant taste and protect the tablet from the atmosphere, or enteric coated for selective disintegration in the gastrointestinal tract.

Liquid dosage forms for oral administration can contain coloring and flavoring to increase patient acceptance.

In general, water, a suitable oil, saline, aqueous dextrose (glucose), and related sugar solutions and glycols such as propylene glycol or polyethylene glycols are suitable carriers for parenteral solutions. Solutions for parenteral administration preferably contain a water soluble salt of the active ingredient, suitable stabilizing agents, and if necessary, buffer substances. Antioxidizing agents such as sodium bisulfite, sodium sulfite, or ascorbic acid, either alone or combined, are suitable stabilizing agents. Also used are citric acid and its salts and sodium EDTA. In addition, parenteral solutions can contain preservatives, such as benzalkonium chloride, methyl- or propyl-paraben, and chlorobutanol.

Suitable pharmaceutical carriers are described in Remington's Pharmaceutical Sciences, Mack Publishing Company, a standard reference text in this field.

Useful pharmaceutical dosage-forms for administration of the compounds of this invention can be illustrated as follows:

Capsules

A large number of unit capsules are prepared by filling standard two-piece hard gelatin capsules each with 10 milligrams of powdered active ingredient, 150 milligrams of lactose, 50 milligrams of cellulose, and 6 milligrams magnesium stearate.

Soft Gelatin Capsules

A mixture of active ingredient in a digestable oil such as soybean oil, cottonseed oil or olive oil is prepared and injected by means of a positive displacement pump into gelatin to form soft gelatin capsules containing 10 milligrams of the active ingredient. The capsules are washed and dried.

Tablets

A large number of tablets are prepared by conventional procedures so that the dosage unit was 10 milligrams of active ingredient, 0.2 milligrams of colloidal silicon dioxide, 5 milligrams of magnesium stearate, 275 milligrams of microcrystalline cellulose, 11 milligrams of starch and 98.8 milligrams of lactose. Appropriate coatings may be applied to increase palatability or delay absorption.

The combination products of this invention, such as the novel α_(v) β₃ antagonist compounds of this invention in combination with an anti-coagulant agent such as warfarin or heparin, or an anti-platelet agent such as aspirin, piroxicam or ticlopidine, or a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, can be in any dosage form, such as those described above, and can also be administered in various ways, as described above.

In a preferred embodiment, the combination products of the invention are formulated together, in a single dosage form (that is, combined together in one capsule, tablet, powder, or liquid, etc.). When the combination products are not formulated together in a single dosage form, the α_(v) β₃ antagonist compounds of this invention and the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent may be administered at the same time (that is, together), or in any order, for example the compounds of this invention are administered first, followed by administration of the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent. When not administered at the same time, preferably the administration of the compound of this invention and any anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent occurs less than about one hour apart, more preferably less than about 30 minutes apart, even more preferably less than about 15 minutes apart, and most preferably less than about 5 minutes apart. Preferably, administration of the combination products of the invention is oral. The terms oral agent, oral inhibitor, oral compound, or the like, as used herein, denote compounds which may be orally administered. Although it is preferable that the α_(v) β₃ antagonist compounds of this invention and the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, and/or thrombolytic agent are both administered in the same fashion (that is, for example, both orally), if desired, they may each be administered in different fashions (that is, for example, one component of the combination product may be administered orally, and another component may be administered intravenously). The dosage of the combination products of the invention may vary depending upon various factors such as the pharmacodynamic characteristics of the particular agent and its mode and route of administration, the age, health and weight of the recipient, the nature and extent of the symptoms, the kind of concurrent treatment, the frequency of treatment, and the effect desired, as described above.

As discussed above, where two or more of the foregoing therapeutic agents are combined or co-administered with the compounds of this invention, generally the amount of each component in a typical daily dosage and typical dosage form may be reduced relative to the usual dosage of the agent when administered alone, in view of the additive or synergistic effect which would be obtained as a result of addition of further agents in accordance with the present invention.

Particularly when provided as a single dosage form, the potential exists for a chemical interaction between the combined active ingredients (for example, a novel compound of this invention and an anti-coagulant such as warfarin or heparin, or a novel compound of this invention and an anti-platelet agent such as aspirin, piroxicam or ticlopidine, or a novel compound of this invention and a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a novel compound of this invention and a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof). For this reason, the preferred dosage forms of the combination products of this invention are formulated such that although the active ingredients are combined in a single dosage form, the physical contact between the active ingredients is minimized (that is, reduced).

In order to minimize contact, one embodiment of this invention where the product is orally administered provides for a combination product wherein one active ingredient is enteric coated. By enteric coating one of the active ingredients, it is possible not only to minimize the contact between the combined active ingredients, but also, it is possible to control the release of one of these components in the gastrointestinal tract such that one of these components is not released in the stomach but rather is released in the intestines. Another embodiment of this invention where oral administration is desired provides for a combination product wherein one of the active ingredients is coated with a sustained-release material which effects a sustained-release throughout the gastrointestinal tract and also serves to minimize physical contact between the combined active ingredients. Furthermore, the sustained-released component can be additionally enteric coated such that the release of this component occurs only in the intestine. Still another approach would involve the formulation of a combination product in which the one component is coated with a sustained and/or enteric release polymer, and the other component is also coated with a polymer such as a low viscosity grade of hydroxypropyl methylcellulose (HPMC) or other appropriate materials as known in the art, in order to further separate the active components. The polymer coating serves to form an additional barrier to interaction with the other component.

Dosage forms of the combination products of the present invention wherein one active ingredient is enteric coated can be in the form of tablets such that the enteric coated component and the other active ingredient are blended together and then compressed into a tablet or such that the enteric coated component is compressed into one tablet layer and the other active ingredient is compressed into an additional layer. Optionally, in order to further separate the two layers, one or more placebo layers may be present such that the placebo layer is between the layers of active ingredients. In addition, dosage forms of the present invention can be in the form of capsules wherein one active ingredient is compressed into a tablet or in the form of a plurality of microtablets, particles, granules or non-perils, which are then enteric coated. These enteric coated microtablets, particles, granules or non-perils are then placed into a capsule or compressed into a capsule along with a granulation of the other active ingredient.

These as well as other ways of minimizing contact between the components of combination products of the present invention, whether administered in a single dosage form or administered in separate forms but at the same time by the same manner, will be readily apparent to those skilled in the art, once armed with the present disclosure.

Pharmaceutical kits useful in, for example, the inhibition of thrombus formation, the prevention of blood clots, and/or the treatment of thromboembolic disorders, which comprise a therapeutically effective amount of a compound according to the method of the present invention along with a therapeutically effective amount of an anti-coagulant agent such as warfarin or heparin, or an antiplatelet agent such as aspirin, piroxicam or ticlopidine, or a thrombin inhibitor such as a boropeptide, hirudin or argatroban, or a thrombolytic agent such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, in one or more sterile containers, are also within the ambit of the present invention. Sterilization of the container may be carried out using conventional sterilization methodology well known to those skilled in the art. The sterile containers of materials may comprise separate containers, or one or more multi-part containers, as exemplified by the UNIVIAL™ two-part container (available from Abbott Labs, Chicago, Ill.), as desired. The compounds according to the method of the invention and the anti-coagulant agent, anti-platelet agent, thrombin inhibitor, thrombolytic agent, and/or combinations thereof, may be separate, or combined into a single dosage form as described above. Such kits may further include, if desired, one or more of various conventional pharmaceutical kit components, such as for example, one or more pharmaceutically acceptable carriers, additional vials for mixing the components, etc., as will be readily apparent to those skilled in the art. Instructions, either as inserts or as labels, indicating quantities of the components to be administered, guidelines for administration, and/or guidelines for mixing the components, may also be included in the kit.

Representative compounds of the present invention are listed in the Tables below.

                                      TABLE 1                                      __________________________________________________________________________      ##STR25##                                                                     Ex.                                                                            No.                                                                               R.sup.1   r R.sup.14                                                                             R.sup.15     MS                                           __________________________________________________________________________     1001                                                                              imidazol-2-yl-                                                                           1 H     H                                                            aminomethyl                                                                 1002                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 Bn                                                aminomethyl                                                                 1003                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-                     aminomethyl       CH.sub.3)                                                 1004                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-                     aminomethyl       CH.sub.3)                                                 1005                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -                        aminomethyl       (4-CH.sub.3)                                              1006                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       pyridinyl)                                                1007                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (3-                                      aminomethyl       pyridinyl)                                                1008                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       pyridinyl)                                                1009                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       thiazolyl)                                                1010                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       thiazolyl)                                                1011                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (5-                                      aminomethyl       thiazolyl)                                                1012                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       isoxazolyl)                                               1013                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       thienyl)                                                  1014                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 CH.sub.2 (5-                                      aminomethyl       isoxazolyl)                                               1015                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 n-Bu                                              aminomethyl                                                                 1016                                                                              imidazol-2-yl                                                                            1 H     NHCO.sub.2 i-Bu                                              aminomethyl                                                                 1017                                                                              imidazol-2-yl-                                                                           1 H     NHCO.sub.2 t-Bu                                              aminomethyl                                                                 1018                                                                              imidazol-2-yl                                                                            1 H     NHCOCH.sub.2 Ph                                              aminomethyl                                                                 1019                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 C.sub.6 H.sub.4 -(2-                            aminomethyl       CH.sub.3)                                                 1020                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 C.sub.6 H.sub.4 -(3-                            aminomethyl       CH.sub.3)                                                 1021                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 C.sub.6 H.sub.4 -(4-                            aminomethyl       CH.sub.3)                                                 1022                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (2-                                             aminomethyl       pyridinyl)                                                1023                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (3-                                             aminomethyl       pyridinyl)                                                1024                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (4-                                             aminomethyl       pyridinyl)                                                1025                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (2-                                             aminomethyl       thiazolyl)                                                1026                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (4-                                             aminomethyl       thiazolyl)                                                1027                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (5-                                             aminomethyl       thiazolyl)                                                1028                                                                              imidazol-2-yl                                                                            1 H     NHCOCH.sub.2 (4-                                             aminomethyl       isoxazol)                                                 1029                                                                              imidazol-2-yl-                                                                           1 H     NHCOCH.sub.2 (2-                                             aminomethyl       thienyl)                                                  1030                                                                              imidazol-2-yl-                                                                           1 H     NHCOn-Bu                                                     aminomethyl                                                                 1031                                                                              imidazol-2-yl                                                                            1 H     NHCOt-Bu                                                     aminomethyl                                                                 1032                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 Ph                                                                               505.2                                           aminomethyl                                                                 1033                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       CH.sub.3)                                                 1034                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       CH.sub.3)                                                 1035                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              aminomethyl       CH.sub.3)                                                 1036                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (2-pyridyl)                                       aminomethyl                                                                 1037                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (3-pyridyl)                                       aminomethyl                                                                 1038                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (4-pyridyl)                                       aminomethyl                                                                 1039                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (2-thiaz-                                         aminomethyl       olyl)                                                     1040                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (3-                                               aminomethyl       thiazolyl)                                                1041                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (4-                                               aminomethyl       isoxazolyl)                                               1042                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2  4-(3,5-                                          aminomethyl       dimethyl)isoxaz                                                                olyl!                                                     1043                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       Br)                                                       1044                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       Br)                                                       1045                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              aminomethyl       Br)                                                       1046                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            aminomethyl                                                                 1047                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            aminomethyl                                                                 1048                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            aminomethyl                                                                 1049                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (2-                                                                              555.2                                           aminomethyl       naphthyl)                                                 1050                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 (1-                                               aminomethyl       naphthyl)                                                 1051                                                                              imidazol-2-yl                                                                            1 H     NHSO.sub.2 CHCHPh                                            aminomethyl                                                                 1052                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 CH.sub.2 Ph                                       aminomethyl                                                                 1053                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 CH.sub.2 CHCHPh                                   aminomethyl                                                                 1054                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 -n-Bu                                             aminomethyl                                                                 1055                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 -i-Bu                                             aminomethyl                                                                 1056                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 -t-Bu                                             aminomethyl                                                                 1057                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHPh                                              aminomethyl                                                                 1058                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-                            aminomethyl       CH.sub.3)                                                 1059                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-                            aminomethyl       CH.sub.3)                                                 1060                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-                            aminomethyl       CH.sub.3)                                                 1061                                                                              imidazol-2-yl-                                                                             H     NHSO.sub.2 NH(2-                                             aminomethyl       pyridyl)                                                  1062                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(3-                                             aminomethyl       pyridyl)                                                  1063                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(4-                                             aminomethyl       pyridyl)                                                  1064                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(2-                                             aminomethyl       thiazolyl)                                                1065                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(4-                                             aminomethyl       thiazolyl)                                                1066                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(4-                                             aminomethyl       isoxazolyl)                                               1067                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2  4-(3,5-                                          aminomethyl       dimethyl)isoxaz                                                                olyl!                                                     1068                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-                            aminomethyl       Br)                                                       1069                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-                            aminomethyl       Br)                                                       1070                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-                            aminomethyl       Br)                                                       1071                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-                            aminomethyl       F)                                                        1072                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-                            aminomethyl       F)                                                        1073                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(2-                                             aminomethyl       naphthyl)                                                 1074                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH(1-                                             aminomethyl       naphthyl)                                                 1075                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHCHCHPh                                          aminomethyl                                                                 1076                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHCH.sub.2 Ph                                     aminomethyl                                                                 1077                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NHCH.sub.2 CHCH-                                  aminomethyl       Ph                                                        1078                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH-n-Bu                                           aminomethyl                                                                 1079                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH-i-Bu                                           aminomethyl                                                                 1080                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 NH-t-Bu                                           aminomethyl                                                                 1081                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 Bn                                                                               510.2                                           aminomethyl                                                                 1082                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-                     aminomethyl       CH.sub.3)                                                 1083                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -                        aminomethyl       (3-CH.sub.3)                                              1084                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -                        aminomethyl       (4-CH.sub.3)                                              1085                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       pyridinyl)                                                1086                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (3-                                      aminomethyl       pyridinyl)                                                1087                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       pyridinyl)                                                1088                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       thiazolyl)                                                1089                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       thiazolyl)                                                1090                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (5-                                      aminomethyl       thiazolyl)                                                1091                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       isoxazolyl)                                               1092                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       thienyl)                                                  1093                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 n-Bu                                              aminomethyl                                                                 1094                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 i-Bu                                              aminomethyl                                                                 1095                                                                              pyridin-2-yl-                                                                            1 H     NHCO.sub.2 t-Bu                                              aminomethyl                                                                 1096                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 Ph                                              aminomethyl                                                                 1097                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 C.sub.6 H.sub.4 -(2-                            aminomethyl       CH.sub.3)                                                 1098                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 C.sub.6 H.sub.4 -                               aminomethyl       (3-CH.sub.3)                                              1099                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 C.sub.6 H.sub.4 -(4-                            aminomethyl       CH.sub.3)                                                 1100                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (2-                                             aminomethyl       pyridinyl)                                                1101                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (3-                                             aminomethyl       pyridinyl)                                                1102                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (4-                                             aminomethyl       pyridinyl)                                                1103                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (2-                                             aminomethyl       thiazolyl)                                                1104                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 -(4-                                            aminomethyl       thiazolyl)                                                1105                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (5-                                             aminomethyl       thiazolyl)                                                1106                                                                           1107                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (4-                                             aminomethyl       isoxazolyl)                                               1108                                                                              pyridin-2-yl-                                                                            1 H     NHCOCH.sub.2 (2-                                             aminomethyl       thienyl)                                                  1109                                                                              pyridin-2-yl-                                                                            1 H     NHCOn-Bu                                                     aminomethyl                                                                 1110                                                                              pyridin-2-yl-                                                                            1 H     NHCOt-Bu                                                     aminomethyl                                                                 1111                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 Ph                                                                               516.1                                           aminomethyl                                                                 1112                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       CH.sub.3)                                                 1113                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       CH.sub.3)                                                 1114                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              aminomethyl       CH.sub.3)                                                 1115                                                                              pyridin-2-yl-                                                                            I H     NHSO.sub.2 (2-pyridyl)                                       aminomethyl                                                                 1116                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (3-pyridyl)                                       aminomethyl                                                                 1117                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (4-pyridyl)                                       aminomethyl                                                                 1118                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (2-                                               aminomethyl       thiazolyl)                                                1119                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (4-                                               aminomethyl       thiazolyl)                                                1120                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (4-                                               aminomethyl       isoxazolyl)                                               1121                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 - 4-(3,5-                                                                        535.1                                           aminomethyl       dimethyl)isoxaz                                                                olyl!                                                     1122                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       Br)                                                       1123                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       Br)                                                       1124                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              aminomethyl       Br)                                                       1125                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            aminomethyl                                                                 1126                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            aminomethyl                                                                 1127                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            aminomethyl                                                                 1128                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (2-                                               aminomethyl       naphthyl)                                                 1129                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 (1-                                               aminomethyl       naphthyl)                                                 1130                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 CHCHPh                                            aminomethyl                                                                 1131                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 CH.sub.2 Ph                                       aminomethyl                                                                 1132                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 -CH.sub.2 CHCH                                    aminomethyl       Ph                                                        1133                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 -n-Bu                                             aminomethyl                                                                 1134                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 -i-Bu                                             aminomethyl                                                                 1135                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 -t-Bu                                             aminomethyl                                                                 1136                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHPh                                              aminomethyl                                                                 1137                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-                            aminomethyl       CH.sub.3)                                                 1138                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-                            aminomethyl       CH.sub.3)                                                 1139                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-                            aminomethyl       CH.sub.3)                                                 1140                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH(2-                                             aminomethyl       pyridyl)                                                  1141                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH(3-                                             aminomethyl       pyridyl)                                                  1142                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH(4-                                             aminomethyl       pyridyl)                                                  1143                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH(2-                                             aminomethyl       thiazolyl)                                                1144                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH-(4-                                            aminomethyl       thiazolyl)                                                1145                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH(4-                                             aminomethyl       isoxazolyl)                                               1146                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 - 4-(3,5-                                         aminomethyl       dimethyl)isoxaz                                                                olyl!                                                     1147                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-                            aminomethyl       Br)                                                       1148                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-                            aminomethyl       Br)                                                       1149                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-                            aminomethyl       Br)                                                       1150                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-                            aminomethyl       F)                                                        1151                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-                            aminomethyl       F)                                                        1152                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH(2-                                             aminomethyl       naphthyl)                                                 1153                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH)1-                                             aminomethyl       naphthyl)                                                 1154                                                                              pyridin-2-yl                                                                             1 H     NHSO.sub.2 NHCHCHPh                                          aminomethyl                                                                 1155                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NHCH.sub.2 Ph                                     aminomethyl                                                                 1156                                                                              pyridin-2-yl                                                                             1 H     NHSO.sub.2 NHCH.sub.2 CHCH                                   aminomethyl       Ph                                                        1157                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH-n-Bu                                           aminomethyl                                                                 1158                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH-i-Bu                                           aminomethyl                                                                 1159                                                                              pyridin-2-yl-                                                                            1 H     NHSO.sub.2 NH-t-Bu                                           aminomethyl                                                                 1160                                                                              tetrahydropyrimidin-                                                                     1 H     NHCOOBn                                                      2-ylaminomethyl                                                             1161                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -                        2-ylaminomethyl   (2-CH.sub.3)                                              1162                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -                        2-ylaminomethyl   (3-CH.sub.3)                                              1163                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -                        2-ylaminomethyl   (4-CH.sub.3)                                              1164                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (2-                                      2-ylaminomethyl   pyridinyl)                                                1165                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (3-                                      2-ylaminomethyl   pyridinyl)                                                1166                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (4-                                      2-ylaminomethyl   pyridinyl)                                                1167                                                                              tetrahydropyrimidin-                                                                       H     NHCO.sub.2 CH.sub.2 (2-                                      2-ylaminomethyl   thiazolyl)                                                1168                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (4-                                      2-ylaminomethyl   thiazolyl)                                                1169                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (5-                                      2-ylaminomethyl   thiazolyl)                                                1170                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (4-                                      2-ylaminomethyl   isoxazolyl)                                               1171                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 CH.sub.2 (2-                                      2-ylaminomethyl   thienyl)                                                  1172                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 n-Bu                                              2-ylaminomethyl                                                             1173                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 i-Bu                                              2-ylaminomethyl                                                             1174                                                                              tetrahydropyrimidin-                                                                     1 H     NHCO.sub.2 t-Bu                                              2-ylaminomethyl                                                             1175                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 Ph                                                                               521.3                                           2-ylaminomethyl                                                             1176                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              2-ylaminomethyl   CH.sub.3)                                                 1177                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              2-ylaminomethyl   CH.sub.3)                                                 1178                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              2-ylaminomethyl   CH.sub.3)                                                 1179                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (2-pyridyl)                                       2-ylaminomethyl                                                             1180                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (3-pyridyl)                                       2-ylaminomethyl                                                             1181                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (4-pyridyl)                                       2-ylaminomethyl                                                             1182                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (2-                                               2-ylaminomethyl   thiazolyl)                                                1183                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (4-                                               2-ylaminomethyl   thiazolyl)                                                1184                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (4-                                               2-ylaminomethyl   isoxazolyl)                                               1185                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 - 4-(3,5-                                         2-ylaminomethyl   dimethyl)isoxaz                                                                olyl!                                                     1186                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              2-ylaminomethyl   Br)                                                       1187                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              2-ylaminomethyl   Br)                                                       1188                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            2-ylaminomethyl                                                             1189                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            2-ylaminomethyl                                                             1190                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            2-ylaminomethyl                                                             1191                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (2-                                               2-ylaminomethyl   naphthyl)                                                 1192                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 (1-                                               2-ylaminomethyl   naphthyl)                                                 1193                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 CHCHPh                                            2-ylaminomethyl                                                             1194                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 CH.sub.2 Ph                                       2-ylaminomethyl                                                             1195                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 CH.sub.2 CHCHPh                                   2-ylaminomethyl                                                             1196                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 -n-Bu                                             2-ylaminomethyl                                                             1197                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 -i-Bu                                             2-ylaminomethyl                                                             1198                                                                              imidazolin-2-yl-                                                                         1 H     NHCOOBn                                                      aminomethyl                                                                 1199                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-                     aminomethyl       CH.sub.3)                                                 1200                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-                     aminomethyl       CH.sub.3)                                                 1201                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-                     aminomethyl       CH.sub.3)                                                 1202                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       pyridinyl)                                                1203                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (3-                                      aminomethyl       pyridinyl)                                                1204                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       pyridinyl)                                                1205                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       thiazolyl)                                                1206                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       thiazolyl)                                                1207                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (5-                                      aminomethyl       thiazolyl)                                                1208                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (4-                                      aminomethyl       isoxazolyl)                                               1209                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 CH.sub.2 (2-                                      aminomethyl       thienyl)                                                  1210                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 n-Bu                                              aminomethyl                                                                 1211                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 i-Bu                                              aminomethyl                                                                 1212                                                                              imidazolin-2-yl-                                                                         1 H     NHCO.sub.2 t-Bu                                              aminomethyl                                                                 1213                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 Ph                                                                               507.3                                           aminomethyl                                                                 1214                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       CH.sub.3)                                                 1215                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       CH.sub.3)                                                 1216                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              aminomethyl       CH.sub.3)                                                 1217                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (2-pyridyl)                                       aminomethyl                                                                 1218                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (3-pyridyl)                                       aminomethyl                                                                 1219                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (4-pyridyl)                                       aminomethyl                                                                 1220                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (2-thiaz-                                         aminomethyl       olyl)                                                     1221                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (4-                                               aminomethyl       isoxazolyl)                                               1222                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 - 4-(3,5-                                         aminomethyl       dimethyl)isoxaz                                                                olyl!                                                     1223                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       Br)                                                       1224                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       Br)                                                       1225                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            aminomethyl                                                                 1226                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            aminomethyl                                                                 1227                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            aminomethyl                                                                 1228                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (2-                                               aminomethyl       naphthyl)                                                 1229                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 (1-                                               aminomethyl       naphthyl)                                                 1230                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 CHCHPh                                            aminomethyl                                                                 1231                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 CH.sub.2 Ph                                       aminomethyl                                                                 1232                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 CH.sub.2 CHCHPh                                   aminomethyl                                                                 1233                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 -n-Bu                                             aminomethyl                                                                 1234                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 -i-Bu                                             aminomethyl                                                                 1235                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1236                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       CH.sub.3)                                                 1237                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       CH.sub.3)                                                 1238                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              aminomethyl       CH.sub.3)                                                 1239                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 (2-pyridyl)                                       aminomethyl                                                                 1240                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 (3-pyridyl)                                       aminomethyl                                                                 1241                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 (4-pyridyl)                                       aminomethyl                                                                 1242                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 (2-                                               aminomethyl       thiazolyl)                                                1243                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 (4-                                               aminomethyl       isoxazolyl)                                               1244                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 - 4-(3,5-                                         aminomethyl       dimethyl)isoxaz                                                                olyl!                                                     1245                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              aminomethyl       Br)                                                       1246                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              aminomethyl       Br)                                                       1247                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            aminomethyl                                                                 1248                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            aminomethyl                                                                 1249                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            aminomethyl                                                                 1250                                                                              benzimidazol-2-yl-                                                                       1 H     NHCO.sub.2 CH.sub.2 Ph                                       aminomethyl                                                                 1251                                                                              benzimidazol-2-yl-                                                                       1 H     NHCO.sub.2 n-Bu                                              aminomethyl                                                                 1252                                                                              benzimidazol-2-yl-                                                                       1 H     NHCO.sub.2 i-Bu                                              aminomethyl                                                                 1253                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1254                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              ylmethyl          CH.sub.3)                                                 1255                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              ylmethyl          CH.sub.3)                                                 1256                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              ylmethyl          CH.sub.3)                                                 1257                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 (2-pyridyl)                                       ylmethyl                                                                    1258                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 (3-pyridyl)                                       ylmethyl                                                                    1259                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 (4-pyridyl)                                       ylmethyl                                                                    1260                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 (2-                                               ylmethyl          thiazolyl)                                                1261                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 (4-                                               ylmethyl          isoxazolyl)                                               1262                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 - 4-(3,5-                                                                        535.1                                           ylmethyl          dimethyl)isoxaz                                                                olyl!                                                     1263                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              ylmethyl          Br)                                                       1264                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              ylmethyl          Br)                                                       1265                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            ylmethyl                                                                    1266                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            ylmethyl                                                                    1267                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            ylmethyl                                                                    1268                                                                              2-aminopyridin-6-                                                                        1 H     NHCO.sub.2 CH.sub.2 Ph                                       ylmethyl                                                                    1269                                                                              2-aminopyridin-6-                                                                        1 H     NHCO.sub.2 n-Bu                                              ylmethyl                                                                    1270                                                                              2-aminopyridin-6-                                                                        1 H     NHCO.sub.2 i-Bu                                              ylmethyl                                                                    1271                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 Ph                                                yl                                                                          1272                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              yl                CH.sub.3)                                                 1273                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              yl                CH.sub.3)                                                 1274                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              yl                CH.sub.3)                                                 1275                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 (2-                                               yl                naphthyl)                                                 1276                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 (1-                                               yl                naphthyl)                                                 1277                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 (biphenyl)                                        yl                                                                          1278                                                                              7-azabenimidazol-2                                                                       1 H     NHSO.sub.2 C.sub.6 H.sub.4 -                                                                569.4                                           yl                (2,4,6-(CH.sub.3).sub.3)                                  1279                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 (2-thienyl)                                       yl                                                                          1280                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 - 4-(3,5-                                         yl                dimethyl)isoxaz                                                                olyl!                                                     1281                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              yl                Br)                                                       1282                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              yl                Br)                                                       1283                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            yl                                                                          1284                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            yl                                                                          1285                                                                              7-azabenimidazol-2-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            yl                                                                          1286                                                                              7-azabenimidazol-2-                                                                      1 H     NHCO.sub.2 CH.sub.2 Ph                                       yl                                                                          1287                                                                              7-azabenimidazol-2-                                                                      1 H     NHCO.sub.2 n-Bu                                              yl                                                                          1288                                                                              7-azabenimidazol-2-                                                                      1 H     NHCO.sub.2 i-Bu                                              yl                                                                          1289                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 Ph                                                                               561.4                                           benzimidazol-2-yl-                                                             aminomethyl                                                                 1290                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              benzimidazol-2-yl-                                                                               CH.sub.3)                                                    aminomethyl                                                                 1291                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              benzimidazol-2-yl-                                                                               CH.sub.3)                                                    aminomethyl                                                                 1292                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              benzimidazol-2-yl-                                                                               CH.sub.3)                                                    aminomethyl                                                                 1293                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 (2-                                               benzimidazol-2-yl-                                                                               naphthyl)                                                    aminomethyl                                                                 1294                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 (1-                                               benzimidazol-2-yl-                                                                               naphthyl)                                                    aminomethyl                                                                 1295                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 (biphenyl)                                        benzimidazol-2-yl-                                                             aminomethyl                                                                 1296                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -                                 benzimidazol-2-yl-                                                                               (2,4,6-(CH.sub.3).sub.3)                                     aminomethyl                                                                 1297                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 (2-thienyl)                                       benzimidazol-2-yl-                                                             aminomethyl                                                                 1298                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 - 4-(3,5-                                         benzimidazol-2-yl-                                                                               dimethyl)isoxaz                                              aminomethyl       olyl!                                                     1299                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              benzimidazol-2-yl-                                                                               Br)                                                          aminomethyl                                                                 1300                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              benzimidazol-2-yl-                                                                               Br)                                                          aminomethyl                                                                 1301                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            benzimidazol-2-yl-                                                             aminomethyl                                                                 1302                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            benzimidazol-2-yl-                                                             aminomethyl                                                                 1303                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            benzimidazol-2-yl-                                                             aminomethyl                                                                 1304                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHCO.sub.2 CH.sub.2 Ph                                       benzimidazol-2-yl-                                                             aminomethyl                                                                 1305                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHCO.sub.2 n-Bu                                              benzimidazol-2-yl-                                                             aminomethyl                                                                 1306                                                                              4,5,6,7-tetrahydro-                                                                      1 H     NHCO.sub.2 i-Bu                                              benzimidazol-2-yl-                                                             aminomethyl                                                                 1307                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 Ph                                                                               549.3                                           tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1308                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              tetrahydro-       CH.sub.3)                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1309                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              tetrahydro-       CH.sub.3)                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1310                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-                              tetrahydro-       CH.sub.3)                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1311                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 (2-                                               tetrahydro-       naphthyl)                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1312                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 (1-                                               tetrahydro-       naphthyl)                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1313                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 (biphenyl)                                        tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1314                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -                                 tetrahydro-       (2,4,6-(CH.sub.3).sub.3)                                     pyrimidin-2-yl-                                                                aminomethyl                                                                 1315                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 (2-thienyl)                                       tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1316                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 - 4-(3,5-                                         tetrahydro-       dimethyl)isoxaz                                              pyrimidin-2-yl-   olyl!                                                        aminomethyl                                                                 1317                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-                              tetrahydro-       Br)                                                          pyrimidin-2-yl-                                                                aminomethyl                                                                 1318                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-                              tetrahydro-       Br)                                                          pyrimidin-2-yl-                                                                aminomethyl                                                                 1319                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                            tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1320                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                            tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1321                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                            tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1322                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHCO.sub.2 CH.sub.2 Ph                                       tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1323                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHCO.sub.2 n-Bu                                              tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1324                                                                              4-oxo-3,4,5,6-                                                                           1 H     NHCO.sub.2 i-Bu                                              tetrahydro-                                                                    pyrimidin-2-yl-                                                                aminomethyl                                                                 1325                                                                              2-iminoazepin-7-                                                                         1 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1326                                                                              1,2-pyrazol-3-                                                                             H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1327                                                                              1,2,4-triazol-5-                                                                         1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1328                                                                              imidazol-4-                                                                              1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1329                                                                              1,3,4-oxadiazol-                                                                         1 H     NHSO.sub.2 Ph                                                2ylaminomethyl                                                              1330                                                                              1,2,4-thiadiazol-5-                                                                      1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1331                                                                              1,2,5-oxadiazol-3-                                                                       1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1332                                                                              1,2,4-oxadiazol-5-                                                                       1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1333                                                                              2-iminoazepin-7-                                                                         1 H     NHSO.sub.2 (4-                                               ylmethyl          isoxazolyl)                                               1334                                                                              1,2-pyrazol-3-                                                                           1 H     NHSO.sub.2 (4-                                               ylaminomethyl     isoxazolyl)                                               1335                                                                              1,2,4-triazol-5-                                                                         1 H     NHSO.sub.2 (4-                                               ylaminomethyl     isoxazolyl)                                               1336                                                                              imidazol-4-                                                                              1 H     NHSO.sub.2 (4-                                               ylaminomethyl     isoxazolyl)                                               1337                                                                              1,3,4-oxadiazol-                                                                         1 H     NHSO.sub.2 (4-                                               2ylaminomethyl    isoxazolyl)                                               1338                                                                              1,2,4-thiadiazol-5-                                                                      1 H     NHSO.sub.2 (4-                                               ylaminomethyl     isoxazolyl)                                               1339                                                                              1.2.5-oxadiazol-3-                                                                       1 H     NHSO.sub.2 (4-                                               ylaminomethyl     isoxazolyl)                                               1340                                                                              1.2.4-oxadiazol-5-                                                                       1 H     NHSO.sub.2 (4-                                               ylaminomethyl     isoxazolyl)                                               1341                                                                              2-iminoazepin-7-                                                                         1 H     NHSO.sub.2 - 4-(3,5-                                         ylmethyl          dimethyl)isoxaz                                                                olyl!                                                     1342                                                                              1,2-pyrazol-3-                                                                           1 H     NHSO.sub.2 - 4-(3,5-                                         ylaminomethyl     dimethyl)isoxaz                                                                olyl!                                                     1343                                                                              1,2,4-triazol-5-                                                                         1 H     NHSO.sub.2 - 4-(3,5-                                         ylaminomethyl     dimethyl)isoxaz                                                                olyl!                                                     1344                                                                              imidazol-4-                                                                              1 H     NHSO.sub.2 - 4-(3,5-                                         ylaminomethyl     dimethyl)isoxaz                                                                olyl!                                                     1345                                                                              1,3,4-oxadiazol-                                                                         1 H     NHSO.sub.2 - 4-(3,5-                                         2ylaminomethyl    dimethyl)isoxaz                                                                olyl!                                                     1346                                                                              1,2,4-thiadiazol-5-                                                                      1 H     NHSO.sub.2 - 4-(3,5-                                         ylaminomethyl     dimethyl)isoxaz                                                                olyl!                                                     1347                                                                              1.2.5-oxadiazol-3-                                                                       1 H     NHSO.sub.2 - 4-(3,5-                                         ylaminomethyl     dimethyl)isoxaz                                                                olyl!                                                     1348                                                                              1.2.4-oxadiazol-5-                                                                       1 H     NHSO.sub.2 - 4-(3,5-                                         ylaminomethyl     dimethyl)isoxaz                                                                olyl!                                                     1349                                                                              imidazol-2-yl-                                                                           1 3-pyridinyl                                                                          H                                                            aminomethyl                                                                 1350                                                                              pyridin-2-                                                                               1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1351                                                                              imidazolin-2-yl-                                                                         1 3-pyridinyl                                                                          H                                                            aminomethyl                                                                 1352                                                                              tetrahydropyrimidin-                                                                     1 3-pyridinyl                                                                          H                                                            2-ylaminomethyl                                                             1353                                                                              benzimidazol-2-yl-                                                                       1 3-pyridinyl                                                                          H                                                            aminomethyl                                                                 1354                                                                              2-aminopyridin-6-                                                                        1 3-pyridinyl                                                                          H                                                            ylmethyl                                                                    1355                                                                              2-iminoazepin-7-                                                                         1 3-pyridinyl                                                                          H                                                            ylmethyl                                                                    1356                                                                              1,2-pyrazol-3-                                                                           1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1357                                                                              1,2,4-triazol-5-                                                                         1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1358                                                                              imidazol-4-                                                                              1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1359                                                                              1,3,4-oxadiazol-                                                                         1 3-pyridinyl                                                                          H                                                            2ylaminomethyl                                                              1360                                                                              1,2,4-thiadiazol-5-                                                                      1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1361                                                                              1,2,5-oxadiazol-3-                                                                       1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1362                                                                              1.2.4-oxadiazol-5-                                                                       1 3-pyridinyl                                                                          H                                                            ylaminomethyl                                                               1363                                                                              imidazol-2-yl-                                                                           1 (3,4- H                                                            aminomethyl methylene-                                                                     dioxy)phenyl                                                    1364                                                                              pyridin-2-                                                                               1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1365                                                                              imidazolin-2-yl-                                                                         1 (3,4- H                                                            aminomethyl methylene-                                                                     dioxy)phenyl                                                    1366                                                                              tetrahydropyrimidin-                                                                     1 (3,4- H                                                            2-ylaminomethyl                                                                            methylene-                                                                     dioxy)phenyl                                                    1367                                                                              benzimidazol-2-yl-                                                                       1 (3,4- H                                                            aminomethyl methylene-                                                                     dioxy)phenyl                                                    1368                                                                              2-aminopyridin-6-                                                                        1 (3,4- H                                                            ylmethyl    methylene-                                                                     dioxy)phenyl                                                    1369                                                                              2-iminoazepin-7-                                                                         1 (3,4- H                                                            ylmethyl    methylene-                                                                     dioxy)phenyl                                                    1370                                                                              1,2-pyrazol-3-                                                                           1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1371                                                                              1,2,4-triazol-5-                                                                         1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1372                                                                              imidazol-4-                                                                              1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1373                                                                              1,3,4-oxadiazol-                                                                         1 (3,4- H                                                            2ylaminomethyl                                                                             methylene-                                                                     dioxy)phenyl                                                    1374                                                                              1,2,4-thiadiazol-5-                                                                      1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1375                                                                              1,2,5-oxadiazol-3-                                                                       1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1376                                                                              1.2.4-oxadiazol-5-                                                                       1 (3,4- H                                                            ylaminomethyl                                                                              methylene-                                                                     dioxy)phenyl                                                    1377                                                                              imidazol-2-yl-                                                                           1 3-pyridinyl                                                                          NHSO.sub.2 Ph                                                aminomethyl                                                                 1378                                                                              pyridin-2-                                                                               1 3-pyridinyl                                                                          NHSO.sub.2 Ph                                                ylaminomethyl                                                               1379                                                                              imidazol-2-yl-                                                                           1 (3,4- NHSO.sub.2 Ph                                                aminomethyl methylene-                                                                     dioxy)phenyl                                                    1380                                                                              pyridin-2-ylamino                                                                        1 (3,4- NHSO.sub.2 Ph                                                            methylene-                                                                     dioxy)phenyl                                                    1381                                                                              imidazol-2-yl-amino                                                                      1 H     NHSO.sub.2 Ph                                             1382                                                                              pyridin-2-ylamino                                                                        1 H     NHSO.sub.2 Ph                                             1383                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 Ph                                                amino                                                                       1384                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 Ph                                                2-ylamino                                                                   1385                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 Ph                                                amino                                                                       1386                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1387                                                                              2-iminoazepin-7-yl                                                                       1 H     NHSO.sub.2 Ph                                             1388                                                                              1,2-pyrazol-3-                                                                           1 H     NHSO.sub.2 Ph                                                ylamino                                                                     1389                                                                              1,2,4-triazol-5-                                                                         1 H     NHSO.sub.2 Ph                                                ylamino                                                                     1390                                                                              imidazol-4-ylamino                                                                       1 H     NHSO.sub.2 Ph                                             1391                                                                              1,3,4-oxadiazol-                                                                         1 H     NHSO.sub.2 Ph                                                2ylaminomethyl                                                              1392                                                                              1,2,4-thiadiazol-5-                                                                      1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1393                                                                              1,2,5-oxadiazol-3-                                                                       1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1394                                                                              1.2.4-oxadiazol-5-                                                                       1 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1395                                                                              imidazol-2-yl-                                                                           1 H     NHSO.sub.2 Ph                                                aminoethyl                                                                  1396                                                                              pyridin-2-                                                                               1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1397                                                                              imidazolin-2-yl-                                                                         1 H     NHSO.sub.2 Ph                                                aminoethyl                                                                  1398                                                                              tetrahydropyrimidin-                                                                     1 H     NHSO.sub.2 Ph                                                2-ylaminoethyl                                                              1399                                                                              benzimidazol-2-yl-                                                                       1 H     NHSO.sub.2 Ph                                                aminoethyl                                                                  1400                                                                              2-aminopyridin-6-                                                                        1 H     NHSO.sub.2 Ph                                                ylethyl                                                                     1401                                                                              2-iminoazepin-7-                                                                         1 H     NHSO.sub.2 Ph                                                ylethyl                                                                     1402                                                                              1,2-pyrazol-3-                                                                           1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1403                                                                              1,2,4-triazol-5-                                                                         1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1404                                                                              imidazol-4-                                                                              1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1405                                                                              1,3,4-oxadiazol-                                                                         1 H     NHSO.sub.2 Ph                                                2ylaminoethyl                                                               1406                                                                              1,2,4-thiadiazol-5-                                                                      1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1407                                                                              1,2,5-oxadiazol-3-                                                                       1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1408                                                                              1,2,4-oxadiazol-5-                                                                       1 H     NHSO.sub.2 Ph                                                ylaminoethyl                                                                1409                                                                              imidazol-2-yl-                                                                           2 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1410                                                                              pyridin-2-                                                                               2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1411                                                                              imidazolin-2-yl-                                                                         2 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1412                                                                              tetrahydropyrimidin-                                                                     2 H     NHSO.sub.2 Ph                                                2-ylaminomethyl                                                             1413                                                                              benzimidazol-2-yl-                                                                       2 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1414                                                                              7-azabenimidazol-2-                                                                      2 H     NHSO.sub.2 Ph                                                yl                                                                          1415                                                                              4,5,6,7-tetrahydro-                                                                      2 H     NHSO.sub.2 Ph                                                benzimidazol-2-yl-                                                             aminomethyl                                                                 1416                                                                              4-oxotetrahydro-                                                                         2 H     NHSO.sub.2 Ph                                                pyrimidin-2-yl-                                                                aminomethyl                                                                 1417                                                                              2-aminopyridin-6-                                                                        2 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1418                                                                              2-iminoazepin-7-                                                                         2 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1419                                                                              1,2-pyrazol-3-                                                                           2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1420                                                                              1,2,4-triazol-5-                                                                         2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1421                                                                              imidazol-4-                                                                              2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1422                                                                              1,3,4-oxadiazol-                                                                         2 H     NHSO.sub.2 Ph                                                2ylaminomethyl                                                              1423                                                                              1,2,4-thiadiazol-5-                                                                      2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1424                                                                              1.2.5-oxadiazol-3-                                                                       2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1425                                                                              1.2.4-oxadiazol-5-                                                                       2 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1426                                                                              imidazol-2-yl-                                                                           0 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1427                                                                              pyridin-2-                                                                               0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1428                                                                              imidazolin-2-yl-                                                                         0 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1429                                                                              tetrahydropyrimidin-                                                                     0 H     NHSO.sub.2 Ph                                                2-ylaminomethyl                                                             1430                                                                              benzimidazol-2-yl-                                                                       0 H     NHSO.sub.2 Ph                                                aminomethyl                                                                 1431                                                                              7-azabenimidazol-2-                                                                      0 H     NHSO.sub.2 Ph                                                yl                                                                          1432                                                                              4,5,6,7-tetrahydro-                                                                      0 H     NHSO.sub.2 Ph                                                benzimidazol-2-yl-                                                             aminomethyl                                                                 1433                                                                              4-oxotetrahydro-                                                                         0 H     NHSO.sub.2 Ph                                                pyrimidin-2-yl-                                                                aminomethyl                                                                 1434                                                                              2-aminopyridin-6-                                                                        0 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1435                                                                              2-iminoazepin-7-                                                                         0 H     NHSO.sub.2 Ph                                                ylmethyl                                                                    1436                                                                              1,2-pyrazol-3-                                                                           0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1437                                                                              1,2,4-triazol-5-                                                                         0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1438                                                                              imidazol-4-                                                                              0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1439                                                                              1,3,4-oxadiazol-                                                                         0 H     NHSO.sub.2 Ph                                                2ylaminomethyl                                                              1440                                                                              1,2,4-thiadiazol-5-                                                                      0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1441                                                                              1,2,5-oxadiazol-3-                                                                       0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1442                                                                              1.2.4-oxadiazol-5-                                                                       0 H     NHSO.sub.2 Ph                                                ylaminomethyl                                                               1443                                                                              benzimidazol-2-                                                                          1 H     NHSO.sub.2 (2,4,6-                                                                          597.4                                           ylaminomethyl     trimethyl                                                                      phenyl)                                                   1444                                                                              2-        1 H     NHSO.sub.2 (2,4,6-                                                                          608.5                                           quinolinylaminometh                                                                              trimethyl                                                    yl                phenyl)                                                   1445                                                                              benzimidazol-2-                                                                          1 H     NHSO.sub.2 (2,4,6-                                                                          611.3                                           ylaminocarbonyl   trimethyl                                                                      phenyl)                                                   1446                                                                              benzimidazol-2-yl                                                                        1 H     NHSO.sub.2 (2,4,6-                                                                          568.5                                                             trimethyl                                                                      phenyl)                                                   1447                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2,4,6-                                                                          561.4                                           ylaminocarbonyl   trimethyl                                                                      phenyl)                                                   1448                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2-                                                                              569.2                                           ylaminocarbonyl   naphthyl)                                                 1449                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2,6-                                                                            587.3/                                          ylaminocarbonyl   dichlorophenyl)                                                                             589.4                                        1450                                                                              pyridin-2-                                                                               1 H     NHSO.sub.2 (2,4,6-                                                                          547.3                                           ylaminomethyl     trimethyl                                                                      phenyl)                                                   1451                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2,4,6-                                                                          547.2                                           ylaminomethyl     trimethyl                                                                      phenyl)                                                   1452                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 biphenyl                                                                         581.2                                           ylaminomethyl                                                               1453                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2  (2,6-                                                                           649.1                                           ylaminomethyl     dichloro-4-                                                                    phenyl)phenyl!                                            1454                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2  (2,6-                                                                           609.2                                           ylaminomethyl     dimethyl-4-                                                                    phenyl)phenyl!                                            1455                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2,6-                                                                            533.2                                           ylaminomethyl     dimethylphenyl)                                           1456                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2-chloro-                                                                       553.2                                           ylaminomethyl     6-methylphenyl)                                           1457                                                                              imidazol-2-                                                                              1 H     NHSO.sub.2 (2,6-                                                                            573.1                                           ylaminomethyl     dichlorophenyl)                                           __________________________________________________________________________

                                      TABLE 2                                      __________________________________________________________________________      ##STR26##                                                                     Ex.                                                                            No. R.sup.1a  r  R.sup.14                                                                           R.sup.15      MS                                          __________________________________________________________________________     2001                                                                               2-aminopyridin-6-yl                                                                      0  H   H                                                         2002                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 Bn                                             2003                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)         2004                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)         2005                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)         2006                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (2-                                                        pyridinyl)                                                2007                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (3-                                                        pyridinyl)                                                2008                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (4-                                                        pyridinyl)                                                2009                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (2-                                                        thiazolyl)                                                2010                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (4-                                                        thiazolyl)                                                2011                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (5-                                                        thiazolyl)                                                2012                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (4-                                                        isoxazolyl)                                               2013                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (2-thienyl)                           2014                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 (5-                                                        isoxazolyl)                                               2015                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 n-Bu                                           2016                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 i-Bu                                           2017                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO.sub.2 t-Bu                                           2018                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCOCH.sub.2 Ph                                           2019                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCOCH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                2020                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCOCH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                2021                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCOCH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                2022                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCO(CH.sub.2).sub.2 Ph                                   2023                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCOn-Bu                                                  2024                                                                               2-aminopyridin-6-yl                                                                      0  H   NHCOt-Bu                                                  2025                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 Ph                                             2026                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2027                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2028                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2029                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (2-pyridyl)                                    2030                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (3-pyridyl)                                    2031                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (4-pyridyl)                                    2032                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (2-thiaz-olyl)                                 2033                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (3-thiazolyl)                                  2034                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (4-isoxazolyl)                                 2035                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2  4-(3,5-                                                            dimethyl) isoxazolyl!                                     2036                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2037                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2038                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)                        2039                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2040                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2041                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2042                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (2-naphthyl)                                   2043                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 (1-naphthyl)                                   2044                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 CHCHPh                                         2045                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 CH.sub.2 Ph                                    2046                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 CH.sub.2 CHCHPh                                2047                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 -n-Bu                                          2048                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 -i-Bu                                          2049                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 -t-Bu                                          2050                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHPh                                           2051                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)                2052                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)                2053                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)                2054                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (2-pyridyl)                                 2055                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (3-pyridyl)                                 2056                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (4-pyridyl)                                 2057                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (2-thiazolyl)                               2058                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (4-thiazolyl)                               2059                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (4-                                                              isoxazolyl)                                               2060                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2  4-(3,5-                                                            dimethyl) isoxazolyl!                                     2061                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-Br)                      2062                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-Br)                      2063                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)                      2064                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-F)                       2065                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)                       2066                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (2-naphthyl)                                2067                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH (1-naphthyl)                                2068                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHCHCHPh                                       2069                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHCH.sub.2 Ph                                  2070                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NHCH.sub.2 CHCHPh                              2071                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH-n-Bu                                        2072                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH-i-Bu                                        2073                                                                               2-aminopyridin-6-yl                                                                      0  H   NHSO.sub.2 NH-t-Bu                                        2074                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 Bn 497.2                                       2075                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)         2076                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)         2077                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)         2078                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (2-                                                        pyridinyl)                                                2079                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (3-                                                        pyridinyl)                                                2080                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (4-                                                        pyridinyl)                                                2081                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (2-                                                        thiazolyl)                                                2082                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (4-                                                        thiazolyl)                                                2083                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (5-                                                        thiazolyl)                                                2084                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (4-                                                        isoxazolyl)                                               2085                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 (2-thienyl)                           2086                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 n-Bu                                           2087                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 i-Bu                                           2088                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCO.sub.2 t-Bu                                           2089                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 Ph                                           2090                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                2091                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                2092                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                2093                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (2-pyridinyl)                                2094                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (3-pyridinyl)                                2095                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (4-pyridinyl)                                2096                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (2-thiazolyl)                                2097                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (4-thiazolyl)                                2098                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (5-thiazolyl)                                2099                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (4-                                                               isoxazolyl)                                               2100                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOCH.sub.2 (2-thienyl)                                  2101                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOn-Bu                                                  2102                                                                               2-aminopyridin-6-yl                                                                      1  H   NHCOt-Bu                                                  2103                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 Ph                                             2104                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2105                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2106                                                                               2-aminopyridin-6-yl                                                                      1      NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2107                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (2-pyridyl)                                    2108                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (3-pyridyl)                                    2109                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (4-pyridyl)                                    2110                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (2-thiazolyl)                                  2111                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (4-thiazolyl)                                  2112                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (4-isoxazolyl)                                 2113                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2114                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2115                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2116                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-Br)                        2117                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2118                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2119                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2120                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (2-naphthyl)                                   2121                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 (1-naphthyl)                                   2122                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 CHCHPh                                         2123                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 CH.sub.2 Ph                                    2124                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2CH.sub.2 CHCHPh                                 2125                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 -n-Bu                                          2126                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 -i-Bu                                          2127                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 -t-Bu                                          2128                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHPh                                           2129                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-CH.sub.3)                2130                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-CH.sub.3)                2131                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-CH.sub.3)                2132                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH (2-pyridyl)                                 2133                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH (3-pyridyl)                                 2134                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH (4-pyridyl)                                 2135                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH (2-thiazolyl)                               2136                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH-(4-                                                              thiazolyl)                                                2137                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH (4-                                                              isoxazolyl)                                               2138                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2139                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(2-Br)                      2140                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-Br)                      2141                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-Br)                      2142                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(3-F)                       2143                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHC.sub.6 H.sub.4 -(4-F)                       2144                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH (2-naphthyl)                                2145                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH) 1-naphthyl)                                2146                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHCHCHPh                                       2147                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHCH.sub.2 Ph                                  2148                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NHCH.sub.2 CHCHPh                              2149                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH-n-Bu                                        2150                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH-i-Bu                                        2151                                                                               2-aminopyridin-6-yl                                                                      1  H   NHSO.sub.2 NH-t-Bu                                        2152                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCOOBn                                                   2153                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)         2154                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)         2155                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)         2156                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (2-                                                        pyridinyl)                                                2157                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (3-                                                        pyridinyl)                                                2158                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (4-                                                        pyridinyl)                                                2159                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (2-                                                        thiazolyl)                                                2160                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (4-                                                        thiazolyl)                                                2161                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (5-                                                        thiazolyl)                                                2162                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (4-                                                        isoxazolyl)                                               2163                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 CH.sub.2 (2-thienyl)                           2164                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 n-Bu                                           2165                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 i-Bu                                           2166                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHCO.sub.2 t-Bu                                           2167                                                                               2-aminoimidazol-5-yl                                                                        H   NHSO.sub.2 Ph                                             2168                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2169                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2170                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2171                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (2-pyridyl)                                    2172                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (3-pyridyl)                                    2173                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (4-pyridyl)                                    2174                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (2-thiazolyl)                                  2175                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (4-thiazolyl)                                  2176                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (4-isoxazolyl)                                 2177                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2178                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2179                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2180                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2181                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2182                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2183                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (2-naphthyl)                                   2184                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 (1-naphthyl)                                   2185                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 CHCHPh                                         2186                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 CH.sub.2 Ph                                    2187                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 CH.sub.2 CHCHPh                                2188                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 -n-Bu                                          2189                                                                               2-aminoimidazol-5-yl                                                                     0  H   NHSO.sub.2 -i-Bu                                          2190                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCOOBn                                                   2191                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)         2192                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)         2193                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)         2194                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (2-                                                        pyridinyl)                                                2195                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (3-                                                        pyridinyl)                                                2196                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (4-                                                        pyridinyl)                                                2197                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (2-                                                        thiazolyl)                                                2198                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (4-                                                        thiazolyl)                                                2199                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (5-                                                        thiazolyl)                                                2200                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (4-                                                        isoxazolyl)                                               2201                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 (2-thienyl)                           2202                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 n-Bu                                           2203                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 i-Bu                                           2204                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 t-Bu                                           2205                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 Ph                                             2206                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2207                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2208                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2209                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (2-pyridyl)                                    2210                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (3-pyridyl)                                    2211                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (4-pyridyl)                                    2212                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (2-thiaz-olyl)                                 2213                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (4-isoxazolyl)                                 2214                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2215                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2216                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2217                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2218                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2219                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2220                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (2-naphthyl)                                   2221                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (1-naphthyl)                                   2222                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 CHCHPh                                         2223                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 CH.sub.2 Ph                                    2224                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 CH.sub.2 CHCHPh                                2225                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 -n-Bu                                          2226                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 -i-Bu                                          2227                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 Ph                                             2228                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2229                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2230                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2231                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (2-pyridyl)                                    2232                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (3-pyridyl)                                    2233                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (4-pyridyl)                                    2234                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (2-thiazolyl)                                  2235                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 (4-isoxazolyl)                                 2236                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2237                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2238                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2239                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2240                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2241                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2242                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 CH.sub.2 Ph                                    2243                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 n-Bu                                           2244                                                                               2-aminoimidazol-5-yl                                                                     1  H   NHCO.sub.2 i-Bu                                           2245                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 Ph                                             2246                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2247                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2248                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2249                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 (2-pyridyl)                                    2250                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 (3-pyridyl)                                    2251                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 (4-pyridyl)                                    2252                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 (2-thiazolyl)                                  2253                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 (4-isoxazolyl)                                 2254                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2255                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2256                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2257                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2258                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2259                                                                               2-aminothiazol-4-yl                                                                      0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2260                                                                               2-aminothiazol-4-yl                                                                      0  H   NHCO.sub.2 CH.sub.2 Ph                                    2261                                                                               2-aminothiazol-4-yl                                                                      0  H   NHCO.sub.2 n-Bu                                           2262                                                                               2-aminothiazol-4-yl                                                                      0  H   NHCO.sub.2 i-Bu                                           2263                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 Ph                                             2264                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                  2265                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                  2266                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                  2267                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 (2-pyridyl)                                    2268                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 (3-pyridyl)                                    2269                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 (4-pyridyl)                                    2270                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 (2-thiazolyl)                                  2271                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 (4-isoxazolyl)                                 2272                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 - 4-(3,5-                                                           dimethyl) isoxazolyl!                                     2273                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                        2274                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                        2275                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                         2276                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                         2277                                                                               2-aminothiazol-4-yl                                                                      1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                         2278                                                                               2-aminothiazol-4-yl                                                                      1  H   NHCO.sub.2 CH.sub.2 Ph                                    2279                                                                               2-aminothiazol-4-yl                                                                      1  H   NHCO.sub.2 n-Bu                                           2280                                                                               2-aminothiazol-4-yl                                                                      1  H   NHCO.sub.2 i-Bu                                           2281                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 Ph                                                 ylmethyl                                                                   2282                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                      ylmethyl                                                                   2283                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                      ylmethyl                                                                   2284                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                      ylmethyl                                                                   2285                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (2-naphthyl)                                       ylmethyl                                                                   2286                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (1-naphthyl                                        ylmethyl                                                                   2287                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (biphenyl)                                         ylmethyl                                                                   2288                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (2,4,6-                                            ylmethyl         trimethylphenyl)                                          2289                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (2-thienyl)                                        ylmethyl                                                                   2290                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 - 4-(3,5-                                          ylmethyl         dimethyl) isoxazolyl!                                     2291                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                            ylmethyl                                                                   2292                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                            ylmethyl                                                                   2293                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                             ylmethyl                                                                   2294                                                                               2-aminopyridin-6                                                                         0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                             ylmethyl                                                                   2295                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                             ylmethyl                                                                   2296                                                                               2-aminopyridin-6-                                                                        0  H   NHCO.sub.2 CH.sub.2 Ph                                        ylmethyl                                                                   2297                                                                               2-aminopyridin-6-                                                                        0  H   NHCO.sub.2 n-Bu                                               ylmethyl                                                                   2298                                                                               2-aminopyridin-6-                                                                        0  H   NHCO.sub.2 i-Bu                                               ylmethyl                                                                   2299                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 Ph                                                 ylmethyl                                                                   2300                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                      ylmethyl                                                                   2301                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                      ylmethyl                                                                   2302                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                      ylmethyl                                                                   2303                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (2-naphthyl)                                       ylmethyl                                                                   2304                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (1-naphthyl)                                       ylmethyl                                                                   2305                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (biphenyl)                                         ylmethyl                                                                   2306                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (2,4,6-                                            ylmethyl         trimethylphenyl)                                          2307                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (2-thienyl)                                        ylmethyl                                                                   2308                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 - 4-(3,5-                                          ylmethyl         dimethyl) isoxazolyl!                                     2309                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                            ylmethyl                                                                   2310                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                            ylmethyl                                                                   2311                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                             ylmethyl                                                                   2312                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                             ylmethyl                                                                   2313                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                             ylmethyl                                                                   2314                                                                               2-aminopyridin-6-                                                                        1  H   NHCO.sub.2 CH.sub.2 Ph                                        ylmethyl                                                                   2315                                                                               2-aminopyridin-6-                                                                        1  H   NHCO.sub.2 n-Bu                                               ylmethyl                                                                   2316                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 Ph                                                 ylcarbonyl                                                                 2317                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                      ylcarbonyl                                                                 2318                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                      ylcarbonyl                                                                 2319                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                      ylcarbonyl                                                                 2320                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (2-naphthyl)                                       ylcarbonyl                                                                 2321                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (1-naphthyl)                                       ylcarbonyl                                                                 2322                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (biphenyl)                                         ylcarbonyl                                                                 2323                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (2,4,6-                                            ylcarbonyl       trimethylphenyl)                                          2324                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 (2-thienyl)                                        ylcarbonyl                                                                 2325                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 - 4-(3,5-                                          ylcarbonyl       dimethyl) isoxazolyl!                                     2326                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                            ylcarbonyl                                                                 2327                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                            ylcarbonyl                                                                 2328                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                             ylcarbonyl                                                                 2329                                                                               2-aminopyridin-6-                                                                        0      NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                             ylcarbonyl                                                                 2330                                                                               2-aminopyridin-6-                                                                        0  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                             ylcarbonyl                                                                 2331                                                                               2-aminopyridin-6-                                                                        0  H   NHCO.sub.2 CH.sub.2 Ph                                        ylcarbonyl                                                                 2332                                                                               2-aminopyridin-6-                                                                        0  H   NHCO.sub.2 n-Bu                                               ylcarbonyl                                                                 2333                                                                               2-aminopyridin-6-                                                                        0  H   NHCO.sub.2 i-Bu                                               ylcarbonyl                                                                 2334                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 Ph                                                 ylcarbonyl                                                                 2335                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                      ylcarbonyl                                                                 2336                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                      ylcarbonyl                                                                 2337                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                      ylcarbonyl                                                                 2338                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (2-naphthyl)                                       ylcarbonyl                                                                 2339                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (1-naphthyl)                                       ylcarbonyl                                                                 2340                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (biphenyl)                                         ylcarbonyl                                                                 2341                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 (2,4,6-                                            ylcarbonyl       trimethylphenyl)                                          2342                                                                               2-aminopyridin-6                                                                         1  H   NHSO.sub.2 (2-thienyl)                                        ylcarbonyl                                                                 2343                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 - 4-(3,5-                                          ylcarbonyl       dimethyl) isoxazolyl!                                     2344                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                            ylcarbonyl                                                                 2345                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                            ylcarbonyl                                                                 2346                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                             ylcarbonyl                                                                 2347                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                             ylcarbonyl                                                                 2348                                                                               2-aminopyridin-6-                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                             ylcarbonyl                                                                 2349                                                                               2-aminopyridin-6-                                                                        1  H   NHCO.sub.2 CH.sub.2 Ph                                        ylcarbonyl                                                                 2350                                                                               2-aminopyridin-6-                                                                        1  H   NHCO.sub.2 n-Bu                                               ylcarbonyl                                                                 2351                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 Ph                                                 ylmethyl                                                                   2352                                                                               2-aminoimidazol-5                                                                        1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-CH.sub.3)                      ylmethyl                                                                   2353                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-CH.sub.3)                      ylmethyl                                                                   2354                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-CH.sub.3)                      ylmethyl                                                                   2355                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 (2-naphthyl)                                       ylmethyl                                                                   2356                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 (1-naphthyl)                                       ylmethyl                                                                   2357                                                                               2-aminoimidazol-5                                                                        1  H   NHSO.sub.2 (biphenyl)                                         ylmethyl                                                                   2358                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 (2,4,6-                                            ylmethyl         trimethylphenyl)                                          2359                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 (2-thienyl)                                        ylmethyl                                                                   2360                                                                               2-aminoimidazol-5                                                                        1  H   NHSO.sub.2 - 4-(3,5-                                          ylmethyl         dimethyl) isoxazolyl!                                     2361                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-Br)                            ylmethyl                                                                   2362                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-Br)                            ylmethyl                                                                   2363                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(2-F)                             ylmethyl                                                                   2364                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(3-F)                             ylmethyl                                                                   2365                                                                               2-aminoimidazol-5-                                                                       1  H   NHSO.sub.2 C.sub.6 H.sub.4 -(4-F)                             ylmethyl                                                                   2366                                                                               2-aminoimidazol-5-                                                                       1  H   NHCO.sub.2 CH.sub.2 Ph                                        ylmethyl                                                                   2367                                                                               2-aminoimidazol-5-                                                                       1  H   NHCO.sub.2 n-Bu                                               ylmethyl                                                                   2368                                                                               2-amino-1,3,4-                                                                           0  H   NHSO.sub.2 Ph                                                 triazol-5-yl-                                                                  carbonyl                                                                   2369                                                                               4-imidazolyl-                                                                            0  H   NHSO.sub.2 Ph                                                 carbonyl                                                                   2370                                                                               2-aminoimidazol-5-                                                                       0  H   NHSO.sub.2 Ph                                                 ylmethyl                                                                   __________________________________________________________________________

                                      TABLE 3                                      __________________________________________________________________________      ##STR27##                                                                     Ex.                                            MS                              No.                                                                               R.sup.1         r R.sup.10 R.sup.14                                                                          R.sup.15      (M + H).sup.+                   __________________________________________________________________________     3001                                                                              2-pyridinylaminomethyl                                                                         0 Cbz      H  NHSO.sub.2 Ph                                 3002                                                                              2-pyridinylaminomethyl                                                                         0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3003                                                                              2-pyridinylaminomethyl                                                                         0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3004                                                                              2-pyridinylaminomethyl                                                                         0 Bn       H  NHSO.sub.2 Ph                                 3005                                                                              2-pyridinylaminomethyl                                                                         0 n-Bu     H  NHSO.sub.2 Ph                                 3006                                                                              2-pyridinylaminomethyl                                                                         0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3007                                                                              2-pyridinylaminomethyl                                                                         0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                 3008                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3009                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3010                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3011                                                                              2-pyridinylaminomethyl                                                                         0 H        H  NHSO.sub.2 Ph                                 3012                                                                              2-pyridinylaminomethyl                                                                         0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3013                                                                              2-pyridinylaminomethyl                                                                         0 COPh     H  NHSO.sub.2 Ph                                 3014                                                                              2-pyridinylaminomethyl                                                                         0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3015                                                                              2-pyridinylaminomethyl                                                                         0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3016                                                                              2-pyridinylaminomethyl                                                                         0 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          679.4                           3017                                                                              2-pyridinylaminomethyl                                                                         0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3018                                                                              2-pyridinylaminomethyl                                                                         0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3019                                                                              2-pyridinylaminomethyl                                                                         0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3020                                                                              2-pyridinylaminomethyl                                                                         0 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3021                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -n-Bu                                                                          H  NRSO.sub.2 -(2,4,6-trimethylphenyl)           3022                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3023                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3024                                                                              2-pyridinylaminomethyl                                                                         0 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          545.5                           3O25                                                                              2-pyridinylaminomethyl                                                                         0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3026                                                                              2-pyridinylaminomethyl                                                                         0 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3027                                                                              2-pyridinylaminomethyl                                                                         0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3028                                                                              2-pyridinylaminomethyl                                                                         0 Cbz      H  NHCbz                                         3029                                                                              2-pyridinylaminomethyl                                                                         0 SO.sub.2 Ph                                                                             H  NHCbz                                         3030                                                                              2-pyridinylaminomethyl                                                                         0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3031                                                                              2-pyridinylaminomethyl                                                                         0 Bn       H  NHCbz                                         3032                                                                              2-pyridinylaminomethyl                                                                         0 n-Bu     H  NHCbz                                         3033                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3034                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3035                                                                              2-pyridinylaminomethyl                                                                         0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3036                                                                              2-pyridinylaminomethyl                                                                         0 H        H  NHCbz                                         3037                                                                              2-pyridinylaminomethyl                                                                         0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3038                                                                              2-pyridinylaminomethyl                                                                         0 COPh     H  NHCbz                                         3039                                                                              2-pyridinylaminomethyl                                                                         0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3040                                                                              2-imidazolylaminomethyl                                                                        0 Cbz      H  NHSO.sub.2 Ph                                 3041                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3042                                                                              2-imidazolylaminomethyl                                                                        0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3043                                                                              2-imidazolylaminomethyl                                                                        0 Bn       H  NHSO.sub.2 Ph                                 3044                                                                              2-imidazolylaminomethyl                                                                        0 n-Bu     H  NHSO.sub.2 Ph                                 3045                                                                              2-imidazolylaminomethyl                                                                        0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3046                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3047                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3048                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3049                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3050                                                                              2-imidazolylaminomethyl                                                                        0 H        H  NHSO.sub.2 Ph 492.3                           3051                                                                              2-imidazolylaminomethyl                                                                        0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3052                                                                              2-imidazolylaminomethyl                                                                        0 COPh     H  NHSO.sub.2 Ph                                 3053                                                                              2-imidazolylaminomethyl                                                                        0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3054                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3055                                                                              2-imidazolylaminomethyl                                                                        0 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          668.4                           3056                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3057                                                                              2-imidazolylaminomethyl                                                                        0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3058                                                                              2-imidazolylaminomethyl                                                                        0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3059                                                                              2-imidazolylaminomethyl                                                                        0 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3060                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3061                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3062                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3063                                                                              2-imidazolylaminomethyl                                                                        0 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          534.4                           3064                                                                              2-imidazolylaminomethyl                                                                        0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3065                                                                              2-imidazolylaminomethyl                                                                        0 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3066                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3067                                                                              2-imidazolylaminomethyl                                                                        0 Cbz      H  NHCbz                                         3068                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 Ph                                                                             H  NHCbz                                         3069                                                                              2-imidazolylaminomethyl                                                                        0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3070                                                                              2-imidazolylaminomethyl                                                                        0 Bn       H  NHCbz                                         3071                                                                              2-imidazolylaminomethyl                                                                        0 n-Bu     H  NHCbz                                         3072                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3073                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3074                                                                              2-imidazolylaminomethyl                                                                        0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3075                                                                              2-imidazolylaminomethyl                                                                        0 H        H  NHCbz                                         3076                                                                              2-imidazolylaminomethyl                                                                        0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3077                                                                              2-imidazolylaminomethyl                                                                        0 COPh     H  NHCbz                                         3078                                                                              2-imidazolylaminomethyl                                                                        0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3079                                                                              2-imidazolinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                 3080                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3081                                                                              2-imidazolinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3082                                                                              2-imidazolinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                 3083                                                                              2-imidazolinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                 3084                                                                              2-imidazolinylaminomethyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3085                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3086                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3087                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3088                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3089                                                                              2-imidazolinylaminomethyl                                                                      0 H        H  NHSO.sub.2 Ph                                 3090                                                                              2-imidazolinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3091                                                                              2-imidazolinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                 3092                                                                              2-imidazolinylaminomethyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3093                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3094                                                                              2-imidazolinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3095                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3096                                                                              2-imidazolinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3097                                                                              2-imidazolinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3098                                                                              2-imidazolinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3099                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3100                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3101                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3102                                                                              2-imidazolinylaminomethyl                                                                      0 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          536.3                           3103                                                                              2-imidazolinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3104                                                                              2-imidazolinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3105                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3106                                                                              2-imidazolinylaminomethyl                                                                      0 Cbz      H  NHCbz                                         3107                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                         3108                                                                              2-imidazolinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3109                                                                              2-imidazolinylaminomethyl                                                                      0 Bn       H  NHCbz                                         3110                                                                              2-imidazolinylaminomethyl                                                                      0 n-Bu     H  NHCbz                                         3111                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3112                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3113                                                                              2-imidazolinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3114                                                                              2-imidazolinylaminomethyl                                                                      0 H        H  NHCbz                                         3115                                                                              2-imidazolinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3116                                                                              2-imidazolinylaminomethyl                                                                      0 COPh     H  NHCbz                                         3117                                                                              2-imidazolinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3118                                                                              2-benzimidazolylaminomethyl                                                                    0 Cbz      H  NHSO.sub.2 Ph                                 3119                                                                              2-benzimidazolylaminomethyl                                                                    0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3120                                                                              2-benzimidazolylaminomethyl                                                                    0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3121                                                                              2-benzimidazolylaminomethyl                                                                    0 Bn       H  NHSO.sub.2 Ph                                 3122                                                                              2-benzimidazolylaminomethyl                                                                    0 n-Bu     H  NHSO.sub.2 Ph                                 3123                                                                              2-benzimidazolylaminomethyl                                                                    0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3124                                                                              2-benzimidazolylaminomethyl                                                                    0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                 3125                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3126                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3127                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3128                                                                              2-benzimidazolylaminomethyl                                                                    0 H        H  NHSO.sub.2 Ph                                 3129                                                                              2-benzimidazolylaminomethyl                                                                    0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3130                                                                              2-benzimidazolylaminomethyl                                                                    0 COPh     H  NHSO.sub.2 Ph                                 3131                                                                              2-benzimidazolylaminomethyl                                                                    0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3132                                                                              2-benzimidazolylaminomethyl                                                                    0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3133                                                                              2-benzimidazolylaminomethyl                                                                    0 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          718.4                           3134                                                                              2-benzimidazolylaminomethyl                                                                    0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3135                                                                              2-benzimidazolylaminomethyl                                                                    0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3136                                                                              2-benzimidazolylaminomethyl                                                                    0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3137                                                                              2-benzimidazolylaminomethyl                                                                    0 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3138                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3139                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3140                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3141                                                                              2-benzimidazolylaminomethyl                                                                    0 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          584.2                           3142                                                                              2-benzimidazolylaminomethyl                                                                    0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3143                                                                              2-benzimidazolylaminomethyl                                                                    0 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3144                                                                              2-benzimidazolylaminomethyl                                                                    0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3145                                                                              2-benzimidazolylaminomethyl                                                                    0 Cbz      H  NHCbz                                         3146                                                                              2-benzimidazolylaminomethyl                                                                    0 SO.sub.2 Ph                                                                             H  NHCbz                                         3147                                                                              2-benzimidazolylaminomethyl                                                                    0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3148                                                                              2-benzimidazolylaminomethyl                                                                    0 Bn       H  NHCbz                                         3149                                                                              2-benzimidazolylaminomethyl                                                                    0 n-Bu     H  NHCbz                                         3150                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3151                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3152                                                                              2-benzimidazolylaminomethyl                                                                    0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3153                                                                              2-benzimidazolylaminomethyl                                                                    0 H        H  NHCbz                                         3154                                                                              2-benzimidazolylaminomethyl                                                                    0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3155                                                                              2-benzimidazolylaminomethyl                                                                    0 COPh     H  NHCbz                                         3156                                                                              2-benzimidazolylaminomethyl                                                                    0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3157                                                                              7-aza-2-benzimidazolyl                                                                         0 Cbz      H  NHSO.sub.2 Ph                                 3158                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3159                                                                              7-aza-2-benzimidazolyl                                                                         0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3160                                                                              7-aza-2-benzimidazolyl                                                                         0 Bn       H  NHSO.sub.2 Ph                                 3161                                                                              7-aza-2-benzimidazolyl                                                                         0 n-Bu     H  NHSO.sub.2 Ph                                 3162                                                                              7-aza-2-benzimidazolyl                                                                         0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3163                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3164                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3165                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3166                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3167                                                                              7-aza-2-benzimidazolyl                                                                         0 H        H  NHSO.sub.2 Ph                                 3168                                                                              7-aza-2-benzimidazolyl                                                                         0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3169                                                                              7-aza-2-benzimidazolyl                                                                         0 COPh     H  NHSO.sub.2 Ph                                 3170                                                                              7-aza-2-benzimidazolyl                                                                         0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3171                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3172                                                                              7-aza-2-benzimidazolyl                                                                         0 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3173                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3174                                                                              7-aza-2-benzimidazolyl                                                                         0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3175                                                                              7-aza-2-benzimidazolyl                                                                         0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3176                                                                              7-aza-2-benzimidazolyl                                                                         0 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3177                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3178                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3179                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3180                                                                              7-aza-2-benzimidazolyl                                                                         0 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3181                                                                              7-aza-2-benzimidazolyl                                                                         0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3182                                                                              7-aza-2-benzimidazolyl                                                                         0 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3183                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3184                                                                              7-aza-2-benzimidazolyl                                                                         0 Cbz      H  NHCbz                                         3185                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 Ph                                                                             H  NHCbz                                         3186                                                                              7-aza-2-benzimidazolyl                                                                         0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3187                                                                              7-aza-2-benzimidazolyl                                                                         0 Bn       H  NHCbz                                         3188                                                                              7-aza-2-benzimidazolyl                                                                         0 n-Bu     H  NHCbz                                         3189                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3190                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3191                                                                              7-aza-2-benzimidazolyl                                                                         0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3192                                                                              7-aza-2-benzimidazolyl                                                                         0 H        H  NHCbz                                         3193                                                                              7-aza-2-benzimidazolyl                                                                         0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3194                                                                              7-aza-2-benzimidazolyl                                                                         0 COPh     H  NHCbz                                         3195                                                                              7-aza-2-benzimidazolyl                                                                         0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3196                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 Cbz      H  NHSO.sub.2 Ph                                 3197                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3198                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3199                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 Bn       H  NHSO.sub.2 Ph                                 3200                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 n-Bu     H  NHSO.sub.2 Ph                                 3201                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3202                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                 3203                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3204                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3205                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3206                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 H        H  NHSO.sub.2 Ph                                 3207                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3208                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 COPh     H  NHSO.sub.2 Ph                                 3209                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3210                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3211                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3212                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3213                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3214                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3215                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3216                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3217                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3218                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3219                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3220                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3221                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3222                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3223                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 Cbz      H  NHCbz                                         3224                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO.sub.2 Ph                                                                             H  NHCbz                                         3225                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3226                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 Bn       H  NHCbz                                         3227                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 n-Bu     H  NHCbz                                         3228                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3229                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3230                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3231                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 H        H  NHCbz                                         3232                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3233                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 COPh     H  NHCbz                                         3234                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3235                                                                              2-pyridinylaminomethyl                                                                         1 Cbz      H  NHSO.sub.2 Ph                                 3236                                                                              2-pyridinylaminomethyl                                                                         1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3237                                                                              2-pyridinylaminomethyl                                                                         1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3238                                                                              2-pyridinylaminomethyl                                                                         1 Bn       H  NHSO.sub.2 Ph                                 3239                                                                              2-pyridinylaminomethyl                                                                         1 n-Bu     H  NHSO.sub.2 Ph                                 3240                                                                              2-pyridinylaminomethyl                                                                         1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3241                                                                              2-pyridinylaminomethyl                                                                         1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                 3242                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3243                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3244                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3245                                                                              2-pyridinylaminomethyl                                                                         1 H        H  NHSO.sub.2 Ph                                 3246                                                                              2-pyridinylaminomethyl                                                                         1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3247                                                                              2-pyridinylaminomethyl                                                                         1 COPh     H  NHSO.sub.2 Ph                                 3248                                                                              2-pyridinylaminomethyl                                                                         1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3249                                                                              2-pyridinylaminomethyl                                                                         1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3250                                                                              2-pyridinylaminomethyl                                                                         1 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3251                                                                              2-pyridinylaminomethyl                                                                         1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3252                                                                              2-pyridinylaminomethyl                                                                         1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3253                                                                              2-pyridinylaminomethyl                                                                         1 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3254                                                                              2-pyridinylaminomethyl                                                                         1 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3255                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3256                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3257                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3258                                                                              2-pyridinylaminomethyl                                                                         1 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3259                                                                              2-pyridinylaminomethyl                                                                         1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3260                                                                              2-pyridinylaminomethyl                                                                         1 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3261                                                                              2-pyridinylaminomethyl                                                                         1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3262                                                                              2-pyridinylaminomethyl                                                                         1 Cbz      H  NHCbz                                         3263                                                                              2-pyridinylaminomethyl                                                                         1 SO.sub.2 Ph                                                                             H  NHCbz                                         3264                                                                              2-pyridinylaminomethyl                                                                         1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3265                                                                              2-pyridinylaminomethyl                                                                         1 Bn       H  NHCbz                                         3266                                                                              2-pyridinylaminomethyl                                                                         1 n-Bu     H  NHCbz                                         3267                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3268                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3269                                                                              2-pyridinylaminomethyl                                                                         1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3270                                                                              2-pyridinylaminomethyl                                                                         1 H        H  NHCbz                                         3271                                                                              2-pyridinylaminomethyl                                                                         1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3272                                                                              2-pyridinylaminomethyl                                                                         1 COPh     H  NHCbz                                         3273                                                                              2-pyridinylaminomethyl                                                                         1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3274                                                                              2-imidazolylaminomethyl                                                                        1 Cbz      H  NHSO.sub.2 Ph                                 3275                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3276                                                                              2-imidazolylaminomethyl                                                                        1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3277                                                                              2-imidazolylaminomethyl                                                                        1 Bn       H  NHSO.sub.2 Ph                                 3278                                                                              2-imidazolylaminomethyl                                                                        1 n-Bu     H  NHSO.sub.2 Ph                                 3279                                                                              2-imidazolylaminomethyl                                                                        1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3280                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3281                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3282                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3283                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3284                                                                              2-imidazolylaminomethyl                                                                        1 H        H  NHSO.sub.2 Ph                                 3285                                                                              2-imidazolylaminomethyl                                                                        1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3286                                                                              2-imidazolylaminomethyl                                                                        1 COPh     H  NHSO.sub.2 Ph                                 3287                                                                              2-imidazolylaminomethyl                                                                        1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3288                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3289                                                                              2-imidazolylaminomethyl                                                                        1 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3290                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3291                                                                              2-imidazolylaminomethyl                                                                        1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3292                                                                              2-imidazolylaminomethyl                                                                        1 Bn       H  NHSO.sub.2 -(2g4,6-trimethylphenyl)           3293                                                                              2-imidazolylaminomethyl                                                                        1 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3294                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3295                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3296                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3297                                                                              2-imidazolylaminomethyl                                                                        1 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3298                                                                              2-imidazolylaminomethyl                                                                        1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3299                                                                              2-imidazolylaminomethyl                                                                        1 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3300                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3301                                                                              2-imidazolylaminomethyl                                                                        1 Cbz      H  NHCbz                                         3302                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 Ph                                                                             H  NHCbz                                         3303                                                                              2-imidazolylaminomethyl                                                                        1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3304                                                                              2-imidazolylaminomethyl                                                                        1 Bn       H  NHCbz                                         3305                                                                              2-imidazolylaminomethyl                                                                        1 n-Bu     H  NHCbz                                         3306                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3307                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3308                                                                              2-imidazolylaminomethyl                                                                        1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3309                                                                              2-imidazolylaminomethyl                                                                        1 H        H  NHCbz                                         3310                                                                              2-imidazolylaminomethyl                                                                        1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3311                                                                              2-imidazolylaminomethyl                                                                        1 COPh     H  NHCbz                                         3312                                                                              2-imidazolylaminomethyl                                                                        1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3313                                                                              2-imidazolinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                 3314                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3315                                                                              2-imidazolinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3316                                                                              2-imidazolinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                 3317                                                                              2-imidazolinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                 3318                                                                              2-imidazolinylaminomethyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3319                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3320                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3321                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3322                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3323                                                                              2-imidazolinylaminomethyl                                                                      1 H        H  NHSO.sub.2 Ph                                 3324                                                                              2-imidazolinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3325                                                                              2-imidazolinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                 3326                                                                              2-imidazolinylaminomethyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3327                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSd2Ph                                       3328                                                                              2-imidazolinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3329                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3330                                                                              2-imidazolinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3331                                                                              2-imidazolinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3332                                                                              2-imidazolinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3333                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3334                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3335                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3336                                                                              2-imidazolinylaminomethyl                                                                      1 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3337                                                                              2-imidazolinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3338                                                                              2-imidazolinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3339                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3340                                                                              2-imidazolinylaminomethyl                                                                      1 Cbz      H  NHCbz                                         3341                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                         3342                                                                              2-imidazolinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3343                                                                              2-imidazolinylaminomethyl                                                                      1 Bn       H  NHCbz                                         3344                                                                              2-imidazolinylaminomethyl                                                                      1 n-Bu     H  NHCbz                                         3345                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3346                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3347                                                                              2-imidazolinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3348                                                                              2-imidazolinylaminomethyl                                                                      1 H        H  NHCbz                                         3349                                                                              2-imidazolinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3350                                                                              2-imidazolinylaminomethyl                                                                      1 COPh     H  NHCbz                                         3351                                                                              2-imidazolinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3352                                                                              2-benzimidazolylaminomethyl                                                                    1 Cbz      H  NHSO.sub.2 Ph                                 3353                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3354                                                                              2-benzimidazolylaminomethyl                                                                    1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3355                                                                              2-benzimidazolylaminomethyl                                                                    1 Bn       H  NHSO.sub.2 Ph                                 3356                                                                              2-benzimidazolylaminomethyl                                                                    1 n-Bu     H  NHSO.sub.2 Ph                                 3357                                                                              2-benzimidazolylaminomethyl                                                                    1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3358                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3359                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3360                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3361                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3362                                                                              2-benzimidazolylaminomethyl                                                                    1 H        H  NHSO.sub.2 Ph                                 3363                                                                              2-benzimidazolylaminomethyl                                                                    1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3364                                                                              2-benzimidazolylaminomethyl                                                                    1 COPh     H  NHSO.sub.2 Ph                                 3365                                                                              2-benzimidazolylaminomethyl                                                                    1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3366                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3367                                                                              2-benzimidazolylaminomethyl                                                                    1 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3368                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3369                                                                              2-benzimidazolylaminomethyl                                                                    1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3370                                                                              2-benzimidazolylaminomethyl                                                                    1 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3371                                                                              2-benzimidazolylaminomethyl                                                                    1 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3372                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3373                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3374                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3375                                                                              2-benzimidazolylaminomethyl                                                                    1 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3376                                                                              2-benzimidazolylaminomethyl                                                                    1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3377                                                                              2-benzimidazolylaminomethyl                                                                    1 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3378                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 -n-BU                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3379                                                                              2-benzimidazolylaminomethyl                                                                    1 Cbz      H  NHCbz                                         3380                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 Ph                                                                             H  NHCbz                                         3381                                                                              2-benzimidazolylaminomethyl                                                                    1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3382                                                                              2-benzimidazolylaminomethyl                                                                    1 Bn       H  NHCbz                                         3383                                                                              2-benzimidazolylaminomethyl                                                                    1 n-Bu     H  NHCbz                                         3384                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3385                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3386                                                                              2-benzimidazolylaminomethyl                                                                    1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3387                                                                              2-benzimidazolylaminomethyl                                                                    1 H        H  NHCbz                                         3388                                                                              2-benzimidazolylaminomethyl                                                                    1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3389                                                                              2-benzimidazolylaminomethyl                                                                    1 COPh     H  NHCbz                                         3390                                                                              2-benzimidazolylaminomethyl                                                                    1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3391                                                                              7-aza-2-benzimidazolyl                                                                         1 Cbz      H  NHSO.sub.2 Ph                                 3392                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3393                                                                              7-aza-2-benzimidazolyl                                                                         1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3394                                                                              7-aza-2-benzimidazolyl                                                                         1 Bn       H  NHSO.sub.2 Ph                                 3395                                                                              7-aza-2-benzimidazolyl                                                                         1 n-Bu     H  NHSO.sub.2 Ph                                 3396                                                                              7-aza-2-benzimidazolyl                                                                         1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3397                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                 3398                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3399                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3400                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3401                                                                              7-aza-2-benzimidazolyl                                                                         1 H        H  NHSO.sub.2 Ph                                 3402                                                                              7-aza-2-benzimidazolyl                                                                         1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3403                                                                              7-aza-2-benzimidazolyl                                                                         1 COPh     H  NHSO.sub.2 Ph                                 3404                                                                              7-aza-2-benzimidazolyl                                                                         1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3405                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3406                                                                              7-aza-2-benzimidazolyl                                                                         1 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3407                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3408                                                                              7-aza-2-benzimidazolyl                                                                         1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3409                                                                              7-aza-2-benzimidazolyl                                                                         1 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3410                                                                              7-aza-2-benzimidazolyl                                                                         1 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3411                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3412                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3413                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3414                                                                              7-aza-2-benzimidazolyl                                                                         1 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3415                                                                              7-aza-2-benzimidazolyl                                                                         1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3416                                                                              7-aza-2-benzimidazolyl                                                                         1 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3417                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3418                                                                              7-aza-2-benzimidazolyl                                                                         1 Cbz      H  NHCbz                                         3419                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 Ph                                                                             H  NHCbz                                         3420                                                                              7-aza-2-benzimidazolyl                                                                         1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3421                                                                              7-aza-2-benzimidazolyl                                                                         1 Bn       H  NHCbz                                         3422                                                                              7-aza-2-benzimidazolyl                                                                         1 n-Bu     H  NHCbz                                         3423                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3424                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3425                                                                              7-aza-2-benzimidazolyl                                                                         1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3426                                                                              7-aza-2-benzimidazolyl                                                                         1 H        H  NHCbz                                         3427                                                                              7-aza-2-benzimidazolyl                                                                         1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3428                                                                              7-aza-2-benzimidazolyl                                                                         1 COPh     H  NHCbz                                         3429                                                                              7-aza-2-benzimidazolyl                                                                         1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                         3430                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 Cbz      H  NHSO.sub.2 Ph                                 3431                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                 3432                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                 3433                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 Bn       H  NHSO.sub.2 Ph                                 3434                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 n-Bu     H  NHSO.sub.2 Ph                                 3435                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                 3436                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                 3437                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3438                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                 3439                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                 3440                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 H        H  NHSO.sub.2 Ph                                 3441                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                 3442                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 COPh     H  NHSO.sub.2 Ph                                 3443                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                 3444                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                 3445                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 Cbz      H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3446                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3447                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3448                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3449                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 n-Bu     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3450                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3451                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3452                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3453                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 H        H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3454                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3455                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 COPh     H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3456                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-trimethylphenyl)           3457                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 Cbz      H  NHCbz                                         3458                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 SO.sub.2 Ph                                                                             H  NHCbz                                         3459                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                         3460                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 Bn       H  NHCbz                                         3461                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 n-Bu     H  NHCbz                                         3462                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                         3463                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                         3464                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                         3465                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 H        H  NHCbz                                         3466                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                         3467                                                                              tetrahydropyrimidin-2-ylaminomethyl                                                            1 COPh     H  NHCbz                                         3468                                                                              imidazol-2-ylaminomethyl                                                                       0 CO.sub.2 Me                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          592.4                           3469                                                                              benzamidazol-2-ylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          674.3                           3470                                                                              benzamidazol-2-ylaminomethyl                                                                   0 CO.sub.2 Me                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          642.3                           3471                                                                              benzamidazol-2-ylaminomethyl                                                                   0 CO.sub.2 Bu                                                                             H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          684.4                           3472                                                                              imidazol-2-ylaminomethyl                                                                       0 CO.sub.2 CH.sub.2 (3-pyr)                                                               H  NHSO.sub.2 -(2,4,6-trimethylphenyl)                                                          669.4                           3473                                                                              imidazol-2-ylaminomethyl                                                                       0 H        H  NHSO.sub.2 -(2,6-trimethylphenyl)                                                            520.3                           3474                                                                              imidazol-2-ylaminomethyl                                                                       0 H        H  NHSO.sub.2 biphenyl                                                                          568.3                           3475                                                                              imidazolin-2-ylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 (2-naphthyl                                                                       678.1                           3476                                                                              imidazolin-2-ylaminomethyl                                                                     0 H        H  NHSO.sub.2 biphenyl                                                                          570.2                           __________________________________________________________________________

                                      TABLE 4                                      __________________________________________________________________________      ##STR28##                                                                     Ex. No.                                                                            R.sup.1      r R.sup.10 R.sup.14                                                                          R.sup.15                                        __________________________________________________________________________     4001                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                   4002                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4003                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4004                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                   4005                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                   4006                                                                               2-pyridinylaminomethyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4007                                                                               2-pyridinylaminomethyl                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4008                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4009                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4010                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4011                                                                               2-pyridinylaminomethyl                                                                      0 H        H  NHSO.sub.2 Ph                                   4012                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4013                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                   4014                                                                               2-pyridinylaminomethyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4015                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4016                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4017                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4018                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4019                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4020                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4021                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4022                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4023                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4024                                                                               2-pyridinylaminomethyl                                                                      0 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4025                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4026                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4027                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4028                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHCbz                                           4029                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                           4030                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4031                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHCbz                                           4032                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHCbz                                           4033                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4034                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4035                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4036                                                                               2-pyridinylaminomethyl                                                                      0 H        H  NHCbz                                           4037                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4038                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHCbz                                           4039                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4040                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 Ph                                   4041                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4042                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4043                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHSO.sub.2 Ph                                   4044                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHSO.sub.2 Ph                                   4045                                                                               2-imidazolylaminomethyl                                                                     0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4046                                                                               2-imidazolylaminomethyl                                                                     0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4047                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4048                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4049                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4050                                                                               2-imidazolylaminomethyl                                                                     0 H        H  NHSO.sub.2 Ph                                   4051                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4052                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHSO.sub.2 Ph                                   4053                                                                               2-imidazolylaminomethyl                                                                     0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4054                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4055                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4056                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4057                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4058                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4059                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4060                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4061                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4062                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4063                                                                               2-imidazolylaminomethyl                                                                     0 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4064                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4065                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4066                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4067                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHCbz                                           4068                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHCbz                                           4069                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4070                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHCbz                                           4071                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHCbz                                           4072                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4073                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4074                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4075                                                                               2-imidazolylaminomethyl                                                                     0 H        H  NHCbz                                           4076                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4077                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHCbz                                           4078                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4079                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHSO.sub.2 Ph                                   4080                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4081                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4082                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 Ph                                   4083                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHSO.sub.2 Ph                                   4084                                                                               2-imidazolinylaminomethyl                                                                   0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4085                                                                               2-imidazolinylaminomethyl                                                                   0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4086                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4087                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4088                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4089                                                                               2-imidazolinylaminomethyl                                                                   0 H        H  NHSO.sub.2 Ph                                   4090                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4091                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHSO.sub.2 Ph                                   4092                                                                               2-imidazolinylaminomethyl                                                                   0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4093                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4094                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4095                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4096                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4097                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4098                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4099                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4100                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4101                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4102                                                                               2-imidazolinylaminomethyl                                                                   0 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4103                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4104                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4105                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4106                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHCbz                                           4107                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHCbz                                           4108                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4109                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHCbz                                           4110                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHCbz                                           4111                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4112                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4113                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4114                                                                               2-imidazolinylaminomethyl                                                                   0 H        H  NHCbz                                           4115                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4116                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHCbz                                           4117                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4118                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHSO.sub.2 Ph                                   4119                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4120                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4121                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHSO.sub.2 Ph                                   4122                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHSO.sub.2 Ph                                   4123                                                                               2-benzimidazolylaminomethyl                                                                 0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4124                                                                               2-benzimidazolylaminomethyl                                                                 0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4125                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4126                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4127                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4128                                                                               2-benzimidazolylaminomethyl                                                                 0 H        H  NHSO.sub.2 Ph                                   4129                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4130                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHSO.sub.2 Ph                                   4131                                                                               2-benzimidazolylaminomethyl                                                                 0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4132                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4133                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4134                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4135                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4136                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4137                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4138                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4139                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4140                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4141                                                                               2-benzimidazolylaminomethyl                                                                 0 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4142                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4143                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4144                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4145                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHCbz                                           4146                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHCbz                                           4147                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4148                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHCbz                                           4149                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHCbz                                           4150                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4151                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4152                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4153                                                                               2-benzimidazolylaminomethyl                                                                 0 H        H  NHCbz                                           4154                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4155                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHCbz                                           4156                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4157                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                   4158                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4159                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4160                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                   4161                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                   4162                                                                               7-aza-2-benzimidazolyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4163                                                                               7-aza-2-benzimidazolyl                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4164                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4165                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4166                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4167                                                                               7-aza-2-benzimidazolyl                                                                      0 H        H  NHSO.sub.2 Ph                                   4168                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4169                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                   4170                                                                               7-aza-2-benzimidazolyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4171                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4172                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4173                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4174                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4175                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4176                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4177                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4178                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4179                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4180                                                                               7-aza-2-benzimidazolyl                                                                      0 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4181                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4182                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4183                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4184                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHCbz                                           4185                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                           4186                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4187                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHCbz                                           4188                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHCbz                                           4189                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4190                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4191                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4192                                                                               7-aza-2-benzimidazolyl                                                                      0 H        H  NHCbz                                           4193                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4194                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHCbz                                           4195                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4196                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4197                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4198                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4199                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4200                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4201                                                                               tetrahydropyrimidin-2-                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4202                                                                               tetrahydropyrimidin-2-                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4203                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4204                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4205                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4206                                                                               tetrahydropyrimidin-2-                                                                      0 H        H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4207                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4208                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4209                                                                               tetrahydropyrimidin-2-                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4210                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4211                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4212                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4213                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4214                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4215                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4216                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4217                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4218                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4219                                                                               tetrahydropyrimidin-2-                                                                      0 H        H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4220                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4221                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4222                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4223                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHCbz                                               ylaminomethyl                                                              4224                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                               ylaminomethyl                                                              4225                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                               ylaminomethyl                                                              4226                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHCbz                                               ylaminomethyl                                                              4227                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHCbz                                               ylaminomethyl                                                              4228                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4229                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4230                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4231                                                                               tetrahydropyrimidin-2-                                                                      0 H        H  NHCbz                                               ylaminomethyl                                                              4232                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                               ylaminomethyl                                                              4233                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHCbz                                               ylaminomethyl                                                              4234                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4235                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                   4236                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4237                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4238                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                   4239                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                   4240                                                                               2-pyridinylaminomethyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4241                                                                               2-pyridinylaminomethyl                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4242                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4243                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4244                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4245                                                                               2-pyridinylaminomethyl                                                                      1 H        H  NHSO.sub.2 Ph                                   4246                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4247                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                   4248                                                                               2-pyridinylaminomethyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4249                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4250                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4251                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4252                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4253                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4254                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4255                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4256                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4257                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4258                                                                               2-pyridinylaminomethyl                                                                      1 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4259                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4260                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4261                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4262                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHCbz                                           4263                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                           4264                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4265                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHCbz                                           4266                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHCbz                                           4267                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4268                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4269                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4270                                                                               2-pyridinylaminomethyl                                                                      1 H        H  NHCbz                                           4271                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4272                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHCbz                                           4273                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4274                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHSO.sub.2 Ph                                   4275                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4276                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4277                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHSO.sub.2 Ph                                   4278                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHSO.sub.2 Ph                                   4279                                                                               2-imidazolylaminomethyl                                                                     1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4280                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                   4281                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4282                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4283                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4284                                                                               2-imidazolylaminomethyl                                                                     1 H        H  NHSO.sub.2 Ph                                   4285                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4286                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHSO.sub.2 Ph                                   4287                                                                               2-imidazolylaminomethyl                                                                     1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4288                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4289                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4290                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4291                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4292                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4293                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4294                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4295                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4296                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4297                                                                               2-imidazolylaminomethyl                                                                     1 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4298                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4299                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4300                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4301                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHCbz                                           4302                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHCbz                                           4303                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4304                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHCbz                                           4305                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHCbz                                           4306                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4307                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4308                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4309                                                                               2-imidazolylaminomethyl                                                                     1 H        H  NHCbz                                           4310                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4311                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHCbz                                           4312                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4313                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHSO.sub.2 Ph                                   4314                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4315                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4316                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHSO.sub.2 Ph                                   4317                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHSO.sub.2 Ph                                   4318                                                                               2-imidazolinylaminomethyl                                                                   1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4319                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -(biphenyl)                                                                    H  NHSO.sub.2 Ph                                   4320                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4321                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4322                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4323                                                                               2-imidazolinylaminomethyl                                                                   1 H        H  NHSO.sub.2 Ph                                   4324                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4325                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHSO.sub.2 Ph                                   4326                                                                               2-imidazolinylaminomethyl                                                                   1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4327                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4328                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4329                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4330                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4331                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4332                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4333                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4334                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4335                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4336                                                                               2-imidazolinylaminomethyl                                                                   1 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4337                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4338                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4339                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4340                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHCbz                                           4341                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHCbz                                           4342                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4343                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHCbz                                           4344                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHCbz                                           4345                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4346                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4347                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4348                                                                               2-imidazolinylaminomethyl                                                                   1 H        H  NHCbz                                           4349                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4350                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHCbz                                           4351                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4352                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHSO.sub.2 Ph                                   4353                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4354                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4355                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHSO.sub.2 Ph                                   4356                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHSO.sub.2 Ph                                   4357                                                                               2-benzimidazolylaminomethyl                                                                 1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4358                                                                               2-benzimidazolylaminomethyl                                                                 1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4359                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4360                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4361                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4362                                                                               2-benzimidazolylaminomethyl                                                                 1 H        H  NHSO.sub.2 Ph                                   4363                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4364                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHSO.sub.2 Ph                                   4365                                                                               2-benzimidazolylaminomethyl                                                                 1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4366                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4367                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4368                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4369                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4370                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4371                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4372                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4373                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4374                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4375                                                                               2-benzimidazolylaminomethyl                                                                 1 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4376                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4377                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4378                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4379                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHCbz                                           4380                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHCbz                                           4381                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4382                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHCbz                                           4383                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHCbz                                           4384                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4385                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4386                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4387                                                                               2-benzimidazolylaminomethyl                                                                 1 H        H  NHCbz                                           4388                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4389                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHCbz                                           4390                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4391                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                   4392                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   4393                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   4394                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                   4395                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                   4396                                                                               7-aza-2-benzimidazolyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   4397                                                                               7-aza-2-benzimidazolyl                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   4398                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4399                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   4400                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   4401                                                                               7-aza-2-benzimidazolyl                                                                      1 H        H  NHSO.sub.2 Ph                                   4402                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   4403                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                   4404                                                                               7-aza-2-benzimidazolyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   4405                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   4406                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4407                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4408                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4409                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4410                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4411                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4412                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4413                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4414                                                                               7-aza-2-benzimidazolyl                                                                      1 H        H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4415                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4416                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4417                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                4418                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHCbz                                           4419                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                           4420                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           4421                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHCbz                                           4422                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHCbz                                           4423                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           4424                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           4425                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           4426                                                                               7-aza-2-benzimidazolyl                                                                      1 H        H  NHCbz                                           4427                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           4428                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHCbz                                           4429                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           4430                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4431                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4432                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4433                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4434                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4435                                                                               tetrahydropyrimidin-2-                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4436                                                                               tetrahydropyrimidin-2-                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4437                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4438                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4439                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4440                                                                               tetrahydropyrimidin-2-                                                                      1 H        H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4441                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4442                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4443                                                                               tetrahydropyrimidin-2-                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4444                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              4445                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4446                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4447                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4448                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4449                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4450                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4451                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4452                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4453                                                                               tetrahydropyrimidin-2-                                                                      1 H        H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4454                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4455                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4456                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                4457                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHCbz                                               ylaminomethyl                                                              4458                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                               ylaminomethyl                                                              4459                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                               ylaminomethyl                                                              4460                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHCbz                                               ylaminomethyl                                                              4461                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHCbz                                               ylaminomethyl                                                              4462                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4463                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4464                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              4465                                                                               tetrahydropyrimidin-2-                                                                      1 H        H  NHCbz                                               ylaminomethyl                                                              4466                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                               ylaminomethyl                                                              4467                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHCbz                                               ylaminomethyl                                                              __________________________________________________________________________

                                      TABLE 5                                      __________________________________________________________________________      ##STR29##                                                                     Ex. No.                                                                            R.sup.1      r R.sup.10a                                                                               R.sup.14                                                                          R.sup.15                                        __________________________________________________________________________     5001                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                   5002                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5003                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5004                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                   5005                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                   5006                                                                               2-pyridinylaminomethyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5007                                                                               2-pyridinylaminomethyl                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5008                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5009                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5010                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5011                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5012                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                   5013                                                                               2-pyridinylaminomethyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5014                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5015                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5016                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5017                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5018                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5019                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5020                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5021                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5022                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5023                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5024                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5025                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5026                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHCbz                                           5027                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                           5028                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5029                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHCbz                                           5030                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHCbz                                           5031                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5032                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5033                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5034                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5035                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHCbz                                           5036                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5037                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 Ph                                   5038                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5039                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5040                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHSO.sub.2 Ph                                   5041                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHSO.sub.2 Ph                                   5042                                                                               2-imidazolylaminomethyl                                                                     0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5043                                                                               2-imidazolylaminomethyl                                                                     0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5044                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5045                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5046                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5047                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5048                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHSO.sub.2 Ph                                   5049                                                                               2-imidazolylaminomethyl                                                                     0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5050                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5051                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5052                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5053                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5054                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5055                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5056                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5057                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5058                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5059                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5060                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5061                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5062                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHCbz                                           5063                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHCbz                                           5064                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5065                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHCbz                                           5066                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHCbz                                           5067                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5068                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5069                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5070                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5071                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHCbz                                           5072                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5073                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHSO.sub.2 Ph                                   5074                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5075                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5076                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 Ph                                   5077                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHSO.sub.2 Ph                                   5078                                                                               2-imidazolinylaminomethyl                                                                   0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5079                                                                               2-imidazolinylaminomethyl                                                                   0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5080                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5081                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5082                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5083                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5084                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHSO.sub.2 Ph                                   5085                                                                               2-imidazolinylaminomethyl                                                                   0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5086                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5087                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5088                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5089                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5090                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5091                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5092                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5093                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5094                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5095                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5096                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5097                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5098                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHCbz                                           5099                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHCbz                                           5100                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5101                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHCbz                                           5102                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHCbz                                           5103                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5104                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5105                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5106                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5107                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHCbz                                           5108                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5109                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHSO.sub.2 Ph                                   5110                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5111                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5112                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHSO.sub.2 Ph                                   5113                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHSO.sub.2 Ph                                   5114                                                                               2-benzimidazolylaminomethyl                                                                 0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5115                                                                               2-benzimidazolylaminomethyl                                                                 0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5116                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5117                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5118                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5119                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5120                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHSO.sub.2 Ph                                   5121                                                                               2-benzimidazolylaminomethyl                                                                 0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5122                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5123                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5124                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5125                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5126                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5127                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5128                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5129                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5130                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5131                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5132                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5133                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5134                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHCbz                                           5135                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHCbz                                           5136                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5137                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHCbz                                           5138                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHCbz                                           5139                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5140                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5141                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5142                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5143                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHCbz                                           5144                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5145                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                   5146                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5147                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5148                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                   5149                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                   5150                                                                               7-aza-2-benzimidazolyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5151                                                                               7-aza-2-benzimidazolyl                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5152                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5153                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5154                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5155                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5156                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                   5157                                                                               7-aza-2-benzimidazolyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5158                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5159                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5160                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5161                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5162                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5163                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5164                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5165                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5166                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5167                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5168                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5169                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5170                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHCbz                                           5171                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                           5172                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5173                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHCbz                                           5174                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHCbz                                           5175                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5176                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5177                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5178                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5179                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHCbz                                           5180                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5181                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5182                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5183                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5184                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5185                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5186                                                                               tetrahydropyrimidin-2-                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5187                                                                               tetrahydropyrimidin-2-                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5188                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5189                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5190                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5191                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5192                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5193                                                                               tetrahydropyrimidin-2-                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5194                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5195                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5196                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5197                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5198                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5199                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5200                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5201                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5202                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5203                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5204                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5205                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5206                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHCbz                                               ylaminomethyl                                                              5207                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                               ylaminomethyl                                                              5208                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                               ylaminomethyl                                                              5209                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHCbz                                               ylaminomethyl                                                              5210                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHCbz                                               ylaminomethyl                                                              5211                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5212                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5213                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5214                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                               ylaminomethyl                                                              5215                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHCbz                                               ylaminomethyl                                                              5216                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5217                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                   5218                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5219                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5220                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                   5221                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                   5222                                                                               2-pyridinylaminomethyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5223                                                                               2-pyridinylaminomethyl                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5224                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5225                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5226                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5227                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5228                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                   5229                                                                               2-pyridinylaminomethyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5230                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5231                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5232                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5233                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5234                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5235                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5236                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5237                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5238                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5239                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5240                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5241                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5242                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHCbz                                           5243                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                           5244                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5245                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHCbz                                           5246                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHCbz                                           5247                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5248                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5249                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5250                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5251                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHCbz                                           5252                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5253                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHSO.sub.2 Ph                                   5254                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5255                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5256                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHSO.sub.2 Ph                                   5257                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHSO.sub.2 Ph                                   5258                                                                               2-imidazolylaminomethyl                                                                     1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5259                                                                               2-imidazolylaminomethyl                                                                     1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5260                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5261                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5262                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5263                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5264                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHSO.sub.2 Ph                                   5265                                                                               2-imidazolylaminomethyl                                                                     1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5266                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5267                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5268                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5269                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5270                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5271                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5272                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5273                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5274                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5275                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5276                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5277                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5278                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHCbz                                           5279                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHCbz                                           5280                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5281                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHCbz                                           5282                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHCbz                                           5283                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5284                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5285                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5286                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5287                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHCbz                                           5288                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5289                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHSO.sub.2 Ph                                   5290                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5291                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5292                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHSO.sub.2 Ph                                   5293                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHSO.sub.2 Ph                                   5294                                                                               2-imidazolinylaminomethyl                                                                   1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5295                                                                               2-imidazolinylaminomethyl                                                                   1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5296                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5297                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5298                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5299                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5300                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHSO.sub.2 Ph                                   5301                                                                               2-imidazolinylaminomethyl                                                                   1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5302                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5303                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5304                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5305                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5306                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5307                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5308                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5309                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5310                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5311                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5312                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5313                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5314                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHCbz                                           5315                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHCbz                                           5316                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5317                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHCbz                                           5318                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHCbz                                           5319                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5320                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5321                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5322                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5323                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHCbz                                           5324                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5325                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHSO.sub.2 Ph                                   5326                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5327                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5328                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHSO.sub.2 Ph                                   5329                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHSO.sub.2 Ph                                   5330                                                                               2-benzimidazolylaminomethyl                                                                 1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5331                                                                               2-benzimidazolylaminomethyl                                                                 1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5332                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5333                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5334                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5335                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5336                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHSO.sub.2 Ph                                   5337                                                                               2-benzimidazolylaminomethyl                                                                 1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5338                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5339                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5340                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5341                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5342                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5343                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5344                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5345                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5346                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5347                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5348                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5349                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5350                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHCbz                                           5351                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHCbz                                           5352                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5353                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHCbz                                           5354                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHCbz                                           5355                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5356                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5357                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5358                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5359                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHCbz                                           5360                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5361                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                   5362                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   5363                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   5364                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                   5365                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                   5366                                                                               7-aza-2-benzimidazolyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   5367                                                                               7-aza-2-benzimidazolyl                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   5368                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5369                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   5370                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   5371                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   5372                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                   5373                                                                               7-aza-2-benzimidazolyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   5374                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   5375                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5376                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5377                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5378                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5379                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5380                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5381                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5382                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5383                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5384                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5385                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                5386                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHCbz                                           5387                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                           5388                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           5389                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHCbz                                           5390                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHCbz                                           5391                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           5392                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           5393                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           5394                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           5395                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHCbz                                           5396                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           5397                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5398                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5399                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5400                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5401                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5402                                                                               tetrahydropyrimidin-2-                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5403                                                                               tetrahydropyrimidin-2-                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5404                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5405                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5406                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5407                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5408                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5409                                                                               tetrahydropyrimidin-2-                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5410                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              5411                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5412                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5413                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5414                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5415                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5416                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5417                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5418                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5419                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5420                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5421                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                5422                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHCbz                                               ylaminomethyl                                                              5423                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                               ylaminomethyl                                                              5424                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                               ylaminomethyl                                                              5425                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHCbz                                               ylaminomethyl                                                              5426                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHCbz                                               ylaminomethyl                                                              5427                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5428                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5429                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              5430                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                               ylaminomethyl                                                              5431                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHCbz                                               ylaminomethyl                                                              5432                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              __________________________________________________________________________

                                      TABLE 6                                      __________________________________________________________________________      ##STR30##                                                                     Ex. No.                                                                            R.sup.1      r R.sup.10a                                                                               R.sup.14                                                                          R.sup.15                                        __________________________________________________________________________     6001                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                   6002                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6003                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6004                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                   6005                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                   6006                                                                               2-pyridinylaminomethyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6007                                                                               2-pyridinylaminomethyl                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6008                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6009                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6010                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6011                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6012                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                   6013                                                                               2-pyridinylaminomethyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6014                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6015                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6016                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6017                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6018                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6019                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6020                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6021                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6022                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6023                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6024                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6025                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6026                                                                               2-pyridinylaminomethyl                                                                      0 Cbz      H  NHCbz                                           6027                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                           6028                                                                               2-pyridinylaminomethyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6029                                                                               2-pyridinylaminomethyl                                                                      0 Bn       H  NHCbz                                           6030                                                                               2-pyridinylaminomethyl                                                                      0 n-Bu     H  NHCbz                                           6031                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6032                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6033                                                                               2-pyridinylaminomethyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6034                                                                               2-pyridinylaminomethyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6035                                                                               2-pyridinylaminomethyl                                                                      0 COPh     H  NHCbz                                           6036                                                                               2-pyridinylaminomethyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6037                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 Ph                                   6038                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6039                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6040                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHSO.sub.2 Ph                                   6041                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHSO.sub.2 Ph                                   6042                                                                               2-imidazolylaminomethyl                                                                     0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6043                                                                               2-imidazolylaminomethyl                                                                     0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6044                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6045                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6046                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6047                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6048                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHSO.sub.2 Ph                                   6049                                                                               2-imidazolylaminomethyl                                                                     0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6050                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6051                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6052                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6053                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6054                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6055                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6056                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6057                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6058                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6059                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6060                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6061                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6062                                                                               2-imidazolylaminomethyl                                                                     0 Cbz      H  NHCbz                                           6063                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 Ph                                                                             H  NHCbz                                           6064                                                                               2-imidazolylaminomethyl                                                                     0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6065                                                                               2-imidazolylaminomethyl                                                                     0 Bn       H  NHCbz                                           6066                                                                               2-imidazolylaminomethyl                                                                     0 n-Bu     H  NHCbz                                           6067                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6068                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6069                                                                               2-imidazolylaminomethyl                                                                     0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6070                                                                               2-imidazolylaminomethyl                                                                     0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6071                                                                               2-imidazolylaminomethyl                                                                     0 COPh     H  NHCbz                                           6072                                                                               2-imidazolylaminomethyl                                                                     0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6073                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHSO.sub.2 Ph                                   6074                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6075                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6076                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 Ph                                   6077                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHSO.sub.2 Ph                                   6078                                                                               2-imidazolinylaminomethyl                                                                   0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6079                                                                               2-imidazolinylaminomethyl                                                                   0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6080                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6081                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6082                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6083                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6084                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHSO.sub.2 Ph                                   6085                                                                               2-imidazolinylaminomethyl                                                                   0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6086                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6087                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6088                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6089                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6090                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6091                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6092                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6093                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6094                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6095                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6096                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6097                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6098                                                                               2-imidazolinylaminomethyl                                                                   0 Cbz      H  NHCbz                                           6099                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 Ph                                                                             H  NHCbz                                           6100                                                                               2-imidazolinylaminomethyl                                                                   0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6101                                                                               2-imidazolinylaminomethyl                                                                   0 Bn       H  NHCbz                                           6102                                                                               2-imidazolinylaminomethyl                                                                   0 n-Bu     H  NHCbz                                           6103                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6104                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6105                                                                               2-imidazolinylaminomethyl                                                                   0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6106                                                                               2-imidazolinylaminomethyl                                                                   0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6107                                                                               2-imidazolinylaminomethyl                                                                   0 COPh     H  NHCbz                                           6108                                                                               2-imidazolinylaminomethyl                                                                   0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6109                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHSO.sub.2 Ph                                   6110                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6111                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6112                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHSO.sub.2 Ph                                   6113                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHSO.sub.2 Ph                                   6114                                                                               2-benzimidazolylaminomethyl                                                                 0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6115                                                                               2-benzimidazolylaminomethyl                                                                 0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6116                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6117                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6118                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6119                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6120                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHSO.sub.2 Ph                                   6121                                                                               2-benzimidazolylaminomethyl                                                                 0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6122                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6123                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6124                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6125                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6126                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6127                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6128                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6129                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6130                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6131                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6132                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6133                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6134                                                                               2-benzimidazolylaminomethyl                                                                 0 Cbz      H  NHCbz                                           6135                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 Ph                                                                             H  NHCbz                                           6136                                                                               2-benzimidazolylaminomethyl                                                                 0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6137                                                                               2-benzimidazolylaminomethyl                                                                 0 Bn       H  NHCbz                                           6138                                                                               2-benzimidazolylaminomethyl                                                                 0 n-Bu     H  NHCbz                                           6139                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6140                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6141                                                                               2-benzimidazolylaminomethyl                                                                 0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6142                                                                               2-benzimidazolylaminomethyl                                                                 0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6143                                                                               2-benzimidazolylaminomethyl                                                                 0 COPh     H  NHCbz                                           6144                                                                               2-benzimidazolylaminomethyl                                                                 0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6145                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHSO.sub.2 Ph                                   6146                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6147                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6148                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHSO.sub.2 Ph                                   6149                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                   6150                                                                               7-aza-2-benzimidazolyl                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6151                                                                               7-aza-2-benzimidazolyl                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6152                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6153                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6154                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6155                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6156                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHSO.sub.2 Ph                                   6157                                                                               7-aza-2-benzimidazolyl                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6158                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6159                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6160                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6161                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6162                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6163                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6164                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6165                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6166                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6167                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6168                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6169                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6170                                                                               7-aza-2-benzimidazolyl                                                                      0 Cbz      H  NHCbz                                           6171                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                           6172                                                                               7-aza-2-benzimidazolyl                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6173                                                                               7-aza-2-benzimidazolyl                                                                      0 Bn       H  NHCbz                                           6174                                                                               7-aza-2-benzimidazolyl                                                                      0 n-Bu     H  NHCbz                                           6175                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6176                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6177                                                                               7-aza-2-benzimidazolyl                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6178                                                                               7-aza-2-benzimidazolyl                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6179                                                                               7-aza-2-benzimidazolyl                                                                      0 COPh     H  NHCbz                                           6180                                                                               7-aza-2-benzimidazolyl                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6181                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6182                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6183                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6184                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6185                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6186                                                                               tetrahydropyrimidin-2-                                                                      0 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6187                                                                               tetrahydropyrimidin-2-                                                                      0 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6188                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6189                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6190                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6191                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6192                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6193                                                                               tetrahydropyrimidin-2-                                                                      0 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6194                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6195                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6196                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6197                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6198                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6199                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6200                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6201                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6202                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6203                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6204                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6205                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6206                                                                               tetrahydropyrimidin-2-                                                                      0 Cbz      H  NHCbz                                               ylaminomethyl                                                              6207                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 Ph                                                                             H  NHCbz                                               ylaminomethyl                                                              6208                                                                               tetrahydropyrimidin-2-                                                                      0 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                               ylaminomethyl                                                              6209                                                                               tetrahydropyrimidin-2-                                                                      0 Bn       H  NHCbz                                               ylaminomethyl                                                              6210                                                                               tetrahydropyrimidin-2-                                                                      0 n-Bu     H  NHCbz                                               ylaminomethyl                                                              6211                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6212                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -i-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6213                                                                               tetrahydropyrimidin-2-                                                                      0 CO.sub.2 -t-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6214                                                                               tetrahydropyrimidin-2-                                                                      0 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                               ylaminomethyl                                                              6215                                                                               tetrahydropyrimidin-2-                                                                      0 COPh     H  NHCbz                                               ylaminomethyl                                                              6216                                                                               tetrahydropyrimidin-2-                                                                      0 SO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6217                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                   6218                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6219                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6220                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                   6221                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                   6222                                                                               2-pyridinylaminomethyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6223                                                                               2-pyridinylaminomethyl                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6224                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6225                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6226                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6227                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6228                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                   6229                                                                               2-pyridinylaminomethyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6230                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6231                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6232                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6233                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6234                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6235                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6236                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6237                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6238                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6239                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6240                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6241                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6242                                                                               2-pyridinylaminomethyl                                                                      1 Cbz      H  NHCbz                                           6243                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                           6244                                                                               2-pyridinylaminomethyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6245                                                                               2-pyridinylaminomethyl                                                                      1 Bn       H  NHCbz                                           6246                                                                               2-pyridinylaminomethyl                                                                      1 n-Bu     H  NHCbz                                           6247                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6248                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6249                                                                               2-pyridinylaminomethyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6250                                                                               2-pyridinylaminomethyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6251                                                                               2-pyridinylaminomethyl                                                                      1 COPh     H  NHCbz                                           6252                                                                               2-pyridinylaminomethyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6253                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHSO.sub.2 Ph                                   6254                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6255                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6256                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHSO.sub.2 Ph                                   6257                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHSO.sub.2 Ph                                   6258                                                                               2-imidazolylaminomethyl                                                                     1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6259                                                                               2-imidazolylaminomethyl                                                                     1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6260                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6261                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6262                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6263                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6264                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHSO.sub.2 Ph                                   6265                                                                               2-imidazolylaminomethyl                                                                     1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6266                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6267                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6268                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6269                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6270                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6271                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6272                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6273                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6274                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6275                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6276                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6277                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6278                                                                               2-imidazolylaminomethyl                                                                     1 Cbz      H  NHCbz                                           6279                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 Ph                                                                             H  NHCbz                                           6280                                                                               2-imidazolylaminomethyl                                                                     1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6281                                                                               2-imidazolylaminomethyl                                                                     1 Bn       H  NHCbz                                           6282                                                                               2-imidazolylaminomethyl                                                                     1 n-Bu     H  NHCbz                                           6283                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6284                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6285                                                                               2-imidazolylaminomethyl                                                                     1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6286                                                                               2-imidazolylaminomethyl                                                                     1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6287                                                                               2-imidazolylaminomethyl                                                                     1 COPh     H  NHCbz                                           6288                                                                               2-imidazolylaminomethyl                                                                     1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6289                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHSO.sub.2 Ph                                   6290                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6291                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6292                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHSO.sub.2 Ph                                   6293                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHSO.sub.2 Ph                                   6294                                                                               2-imidazolinylaminomethyl                                                                   1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6295                                                                               2-imidazolinylaminomethyl                                                                   1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6296                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6297                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6298                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6299                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6300                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHSO.sub.2 Ph                                   6301                                                                               2-imidazolinylaminomethyl                                                                   1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6302                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6303                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6304                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6305                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6306                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6307                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6308                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6309                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6310                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6311                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6312                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6313                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6314                                                                               2-imidazolinylaminomethyl                                                                   1 Cbz      H  NHCbz                                           6315                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 Ph                                                                             H  NHCbz                                           6316                                                                               2-imidazolinylaminomethyl                                                                   1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6317                                                                               2-imidazolinylaminomethyl                                                                   1 Bn       H  NHCbz                                           6318                                                                               2-imidazolinylaminomethyl                                                                   1 n-Bu     H  NHCbz                                           6319                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6320                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6321                                                                               2-imidazolinylaminomethyl                                                                   1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6322                                                                               2-imidazolinylaminomethyl                                                                   1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6323                                                                               2-imidazolinylaminomethyl                                                                   1 COPh     H  NHCbz                                           6324                                                                               2-imidazolinylaminomethyl                                                                   1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6325                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHSO.sub.2 Ph                                   6326                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6327                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6328                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHSO.sub.2 Ph                                   6329                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHSO.sub.2 Ph                                   6330                                                                               2-benzimidazolylaminomethyl                                                                 1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6331                                                                               2-benzimidazolylaminomethyl                                                                 1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6332                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6333                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6334                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6335                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6336                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHSO.sub.2 Ph                                   6337                                                                               2-benzimidazolylaminomethyl                                                                 1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6338                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6339                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6340                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6341                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6342                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6343                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6344                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6345                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6346                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6347                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6348                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6349                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6350                                                                               2-benzimidazolylaminomethyl                                                                 1 Cbz      H  NHCbz                                           6351                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 Ph                                                                             H  NHCbz                                           6352                                                                               2-benzimidazolylaminomethyl                                                                 1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6353                                                                               2-benzimidazolylaminomethyl                                                                 1 Bn       H  NHCbz                                           6354                                                                               2-benzimidazolylaminomethyl                                                                 1 n-Bu     H  NHCbz                                           6355                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6356                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6357                                                                               2-benzimidazolylaminomethyl                                                                 1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6358                                                                               2-benzimidazolylaminomethyl                                                                 1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6359                                                                               2-benzimidazolylaminomethyl                                                                 1 COPh     H  NHCbz                                           6360                                                                               2-benzimidazolylaminomethyl                                                                 1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6361                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHSO.sub.2 Ph                                   6362                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                   6363                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                   6364                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHSO.sub.2 Ph                                   6365                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                   6366                                                                               7-aza-2-benzimidazolyl                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                   6367                                                                               7-aza-2-benzimidazolyl                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                   6368                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6369                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                   6370                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                   6371                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                   6372                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHSO.sub.2 Ph                                   6373                                                                               7-aza-2-benzimidazolyl                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                   6374                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                   6375                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6376                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6377                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6378                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6379                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6380                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6381                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6382                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6383                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6384                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6385                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                                            trimethylphenyl)                                6386                                                                               7-aza-2-benzimidazolyl                                                                      1 Cbz      H  NHCbz                                           6387                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                           6388                                                                               7-aza-2-benzimidazolyl                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                           6389                                                                               7-aza-2-benzimidazolyl                                                                      1 Bn       H  NHCbz                                           6390                                                                               7-aza-2-benzimidazolyl                                                                      1 n-Bu     H  NHCbz                                           6391                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                           6392                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                           6393                                                                               7-aza-2-benzimidazolyl                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                           6394                                                                               7-aza-2-benzimidazolyl                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                           6395                                                                               7-aza-2-benzimidazolyl                                                                      1 COPh     H  NHCbz                                           6396                                                                               7-aza-2-benzimidazolyl                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                           6397                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6398                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6399                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6400                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6401                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6402                                                                               tetrahydropyrimidin-2-                                                                      1 COCH.sub.2 (3-indolyl)                                                                  H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6403                                                                               tetrahydropyrimidin-2-                                                                      1 SO2-(biphenyl)                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6404                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6405                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6406                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6407                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6408                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6409                                                                               tetrahydropyrimidin-2-                                                                      1 cyclopropylmethyl                                                                       H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6410                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 Ph                                       ylaminomethyl                                                              6411                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6412                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6413                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6414                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6415                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6416                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6417                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6418                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6419                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6420                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6421                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHSO.sub.2 -(2,4,6-                                 ylaminomethyl              trimethylphenyl)                                6422                                                                               tetrahydropyrimidin-2-                                                                      1 Cbz      H  NHCbz                                               ylaminomethyl                                                              6423                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 Ph                                                                             H  NHCbz                                               ylaminomethyl                                                              6424                                                                               tetrahydropyrimidin-2-                                                                      1 CO(CH.sub.2).sub.2 Ph                                                                   H  NHCbz                                               ylaminomethyl                                                              6425                                                                               tetrahydropyrimidin-2-                                                                      1 Bn       H  NHCbz                                               ylaminomethyl                                                              6426                                                                               tetrahydropyrimidin-2-                                                                      1 n-Bu     H  NHCbz                                               ylaminomethyl                                                              6427                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6428                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -i-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6429                                                                               tetrahydropyrimidin-2-                                                                      1 CO.sub.2 -t-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              6430                                                                               tetrahydropyrimidin-2-                                                                      1 (CH.sub.2).sub.4 NH.sub.2                                                               H  NHCbz                                               ylaminomethyl                                                              6431                                                                               tetrahydropyrimidin-2-                                                                      1 COPh     H  NHCbz                                               ylaminomethyl                                                              6432                                                                               tetrahydropyrimidin-2-                                                                      1 SO.sub.2 -n-Bu                                                                          H  NHCbz                                               ylaminomethyl                                                              __________________________________________________________________________ 

What is claimed is:
 1. A compound of Formula I:

    R.sup.1 --Q--W--X--Y                                       (I)

and pharmaceutically acceptable salt forms thereof, wherein: Q is selected from ##STR31## A is selected from --N(R¹⁰)--, --C(R¹¹)-- or --O--; A¹ is selected from --O-- or --N(R¹⁰)--; Z is a spiro-fused 4-7 membered ring system (including the sprio atom) containing 0-2 heteroatoms selected from O, S, or N, said ring system optionally being substituted on carbon with keto, or being substituted on carbon or nitrogen independently with 0-2 R⁹ or R¹⁰ or R^(10a) ; R¹ is selected from: ##STR32## B is independently selected from --CH₂ --, --O--, --N(R²)--, or --C(═O)--; B¹ is independently selected from --CH₂ -- or --N(R³)--; D is --N(R²)--, --O--, --S--, --C(═O)-- or --SO₂ --; E-F is --C(R⁴)═C(R⁵)--, --N═C(R⁴)--, --C(R⁴)═N--, or --C(R⁴)₂ C(R⁵)₂ --; J, K, L and M are independently selected from --C(R⁴)--, --C(R⁵)-- or --N--, provided that at least one of J, K, L and M is not --N--; R² is selected from: H, C₁ -₆ alkyl, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl; (C₁ -C₆ alkyl)aminocarbonyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, heteroaryl(C₁ -C₆ alkyl)carbonyl, heteroarylcarbonyl, aryl C₁ -C₆ alkyl, (C₁ -C₆ alkyl)carbonyl, arylcarbonyl, C₁ -C₆ alkylsulfonyl, arylsulfonyl, aryl(C₁ -C₆ alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C₁ -C₆ alkyl)sulfonyl, aryloxycarbonyl, aryl(C₁ -C₆ alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents independently selected from the group consisting of C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, CF₃, and nitro; R³ is selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₁ -C₆ alkyl)-; R⁴ and R⁵ are independently selected from: H C₁ -C₄ alkoxy, NR² R³, halogen, NO₂, CN, CF₃, C₁ -C₆ alkyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl (C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl, arylcarbonyl; alternatively, when substituents on adjacent atoms, R⁴ and R⁵ can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups independently selected from: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, cyano, amino, CF₃, or NO₂ ; R⁶ is selected from: H, C₁ -C₄ alkyl, or benzyl; R⁷ and R⁸ are independently selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₀ -C₆ alkyl)-; U is selected from:--N(R⁶) (CH₂)_(n) --, --N(R⁶) (CH₂)_(m) O--, --N(R⁶) (CH₂)_(m) N(R⁷)-- --N(R⁶) (CH₂)_(n) S(O)_(p) -- --N(R⁶)C(═O) (CH₂)_(n) --; --N(R⁶) (CH₂)_(m) C(═O)--; V is selected from:--(CH₂)_(n) --, --(CH₂)_(m) O--(CH₂)_(n) --, --(CH₂)_(m) N(R⁷) (CH₂)_(n) --, --(CH₂)_(n) S(O)_(p) (CH₂)_(n) --, --(CH₂)_(m) N(R⁷)C(═O) (CH₂)_(n) --, --(CH₂)_(n) C(═O)N(R⁷) (CH₂)_(n) --, --(CH₂)_(n) C(═O) (CH₂)_(n) --; R⁹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl; R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with ₀₋₁ R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl; W is selected from:C₁ -C₄ alkylene, --(C(R¹²)₂)_(q) O(C(R¹²)₂)_(q) --, --(C(R¹²)₂)_(q) C(═O) (C(R¹²)₂)_(q) --, --(C(R¹²)₂)_(q) C(═O)N(R¹³)--, --C(═O)--N(R¹³)--(C(R¹²)₂)_(q) --; X is --(C(R¹²)₂)_(q) C(R¹²) (R¹⁴)--C(R¹²) (R¹⁵)--; alternatively, W and X can be taken together to be ##STR33## R¹² is selected from H, C₁ -C₆ alkyl, C₂ -C₆ alkenyl, C₂ -C₆ alkynyl, C₃ -C₇ cycloalkyl, C₄ -C₁₀ cycloalkylalkyl, (C₁ -C₄ alkyl)carbonyl, aryl, or aryl(C₁ -C₆ alkyl)-; R¹³ is selected from H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkylmethyl, or aryl(C₁ -C₆ alkyl)- R¹⁴ is selected from:H, C₁ -C₆ alkylthio(C₁ -C₆ alkyl)-, aryl(C₁ -C₁₀ alkylthioalkyl)-, aryl(C₁ -C₁₀ alkoxyalkyl)-, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₆ hydroxyalkyl, C₂ -C₁₀ alkenyl, C₂ -C₁₀ alkynyl, C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl (C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, or CONR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-1 R¹⁶ or 0-2 R¹¹ ; R¹⁵ is selected from:H, R¹⁶, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₁₀ alkylaminoalkyl, C₁ -C₁₀ dialkylaminoalkyl, (C₁ -C₁₀ alkyl)carbonyl, aryl(C₀ -C₆ alkyl)carbonyl, C₁ -C₁₀ alkenyl, C₁ -C₁₀ alkynyl, C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl (C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, SO₂ R¹⁷, or SO₂ NR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-2 R¹¹ ; Y is selected from:--COR¹⁹, --SO₃ H, --PO₃ H, tetrazolyl, --CONHNHSO₂ CF₃, --CONHSO₂ R¹⁷, --CONHSO₂ NHR¹⁷, --NHCOCF₃, --NHCONHSO₂ R¹⁷, --NHSO₂ R¹⁷, --OPO₃ H₂, --OSO₃ H, --PO₃ H₂, --SO₃ H, --SO₂ NHCOR¹⁷, --SO₂ NHCO₂ R¹⁷, ##STR34## R¹⁶ is selected from: --N(R²⁰)--C(═O)--O--R¹⁷, --N(R²⁰)--C(═O)--R¹⁷, --N(R²⁰)--C(═O)--NH--R¹⁷, --N(R²⁰)SO₂ --R¹⁷, or --N(R²⁰)SO₂ --NR²⁰ R¹⁷ ; R¹⁷ is selected from:C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl) heteroaryl, arylaryl (C₁ -C₆ alkyl)-, heteroarylaryl (C₁ -C₆ alkyl)-, arylheteroaryl (C₁ -C₆ alkyl)-, heteroarylheteroaryl (C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ; R¹⁸ is selected from:H, --C(═O)--O--R¹⁷, --C(═O)--R¹⁷, --C(═O)--NH--R¹⁷, --SO₂ --R¹⁷, or --SO₂ --NR²⁰ R¹⁷ ; R¹⁹ is selected from:hydroxy, C₁ -C₁₀ alkyloxy, C₃ -C₁₁ cycloalkyloxy, aryloxy, aryl(C₁ -C₆ alkoxy)-, C₃ -C₁₀ alkylcarbonyloxyalkyloxy, C₃ -C₁₀ alkoxycarbonyloxyalkyloxy, C₂ -C₁₀ alkoxycarbonylalkyloxy, C₅ -C₁₀ cycloalkylcarbonyloxyalkyloxy, C₅ -C₁₀ cycloalkoxycarbonyloxyalkyloxy, C₅ -C₁₀ cycloalkoxycarbonylalkyloxy, C₇ -C₁₁ aryloxycarbonylalkyloxy, C₈ -C₁₂ aryloxycarbonyloxyalkyloxy, C₈ -C₁₂ arylcarbonyloxyalkyloxy, C₅ -C₁₀ alkoxyalkylcarbonyloxyalkyloxy, C₅ -C₁₀ ( 5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C₁₀ -C₁₄ (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R¹¹) (R¹²)N--(C₁ -C₁₀ alkoxy)-; R²⁰ is selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl (C₁ -C₆ alkyl)-; m is 1-2; n is 0-2; p is 0-2; q is 0-2; and r is 0-2;provided that: n, q, and r are chosen such that the number of in-chain atoms between R¹ and Y is in the range of 8-18.
 2. A compound of claim 1 of the Formula I:

    R.sup.1 --Q--W--X--Y                                       (I)

and pharmaceutically acceptable salt forms thereof wherein: Q is selected from: ##STR35## R¹ is selected from: ##STR36## D is --N(R²)--, --O--, --S--, --C(═O)-- or --SO₂ --; E-F is --C(R⁴)═C(R⁵)--, --N═C(R⁴)--, --C(R⁴)═N--, or --C(R⁴)₂ C(R⁵)₂ --; J, K, L and M are independently selected from --C(R⁴)--, --C(R⁵)-- or --N--, provided that at least one of J, K, L and M is not --N--; R² is selected from: H, C₁ -C₆ alkyl, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl; (C₁ -C₆ alkyl)aminocarbonyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, heteroaryl(C₁ -C₆ alkyl)carbonyl, heteroarylcarbonyl, aryl (C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl) carbonyl, arylcarbonyl, C₁ -C₆ alkylsulfonyl, arylsulfonyl, aryl(C₁ -C₆ alkyl)sulfonyl, heteroarylsulfonyl, heteroaryl(C₁ -C₆ alkyl)sulfonyl, aryloxycarbonyl, or aryl(C₁ -C₆ alkoxy)carbonyl, wherein said aryl groups are substituted with 0-2 substituents independently selected from the group consisting of C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, CF₃, and nitro; R³ is selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₁ -C₆ alkyl)-; R⁴ and R⁵ are independently selected from: H, C₁ -C₄ alkoxy, NR² R³, halogen, NO₂, CN, CF₃, C₁ -C₆ alkyl, C₃ -C₆ alkenyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)carbonyl, (C₁ -C₆ alkoxy)carbonyl, arylcarbonyl, or alternatively, when substituents on adjacent atoms, R⁴ and R⁵ can be taken together with the carbon atoms to which they are attached to form a 5-7 membered carbocyclic or 5-7 membered heterocyclic aromatic or non-aromatic ring system, said carbocyclic or heterocyclic ring being optionally substituted with 0-2 groups independently selected from: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, halo, cyano, amino, CF₃, or NO₂ ; R⁶ is selected from: H, C₁ -C₄ alkyl, or benzyl; R⁷ and R⁸ are independently selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl(C₀ -C₆ alkyl)-; U is selected from:--N(R⁶) (CH₂)_(n) --, --N(R⁶) (CH₂)_(m) O--, --N(R⁶) (CH₂)_(m) N(R⁷)-- --N(R⁶) (CH₂)_(n) S(O)_(p--) --N(R⁶) C(═O) (CH₂)_(n--;) V is selected from:--(CH₂)_(n) --, --(CH₂)_(m) O--(CH₂)_(n) --, --(CH₂)_(m) N(R⁷) (CH₂)_(n) --, --(CH₂)_(n) S(O)_(p) (CH₂)_(n) --, --(CH₂)_(m) N(R⁷)C(═O) (CH₂)_(n) --, --(CH₂)_(n) C(═O)N(R⁷) (CH₂)_(n) --, --(CH₂)_(n) C(═O) (CH₂)_(n) --; R⁹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl; R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl; W is selected from:C₁ -C₄ alkylene, --(C(R¹²)₂)_(q) O(C(R¹²)₂)_(q) --, --(C(R¹²)₂)_(q) C(═O) (C(R¹²)₂)_(q) --, --(C(R¹²)₂)_(q) C(═O)N(R¹³)--, --C(═O)--N(R¹³)--(C(R¹²)₂)_(q) --; X is --(C(R¹²)₂)_(q) C(R¹²) (R¹⁴)--C(R¹²) (R¹⁵)--; alternatively, W and X can be taken together to be ##STR37## R¹² is selected from H, C₁ -C₆ alkyl, C₂ -C₆ alkenyl, C₂ -C₆ alkynyl, C₃ -C₇ cycloalkyl, C₄ -C₁₀ cycloalkylalkyl, (C₁ -C₄ alkyl)carbonyl, aryl, or aryl(C₁ -C₆ alkyl)-; R¹³ is selected from H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkylmethyl, or aryl(C₁ -C₆ alkyl)-; R¹⁴ is selected from:H, C₁ -C₆ alkylthio(C₁ -C₆ alkyl)-, aryl(C₁ -C₁₀ alkylthioalkyl)-, aryl (C₁ -C₁₀ alkoxyalkyl)-, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₆ hydroxyalkyl, C₂ -C₁₀ alkenyl, C₂ -C₁₀ alkynyl, C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl (C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, or CONR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-1 R¹⁶ or 0-2 R¹¹ ; R¹⁵ is selected from: H, R¹⁶, C₁ -C₁₀ alkyl, C₁ -C₁₀ alkoxyalkyl, C₁ -C₁₀ alkylaminoalkyl, C₁ -C₁₀ dialkylaminoalkyl, (C₁ -C₁₀ alkyl)carbonyl, aryl(C₀ -C₆ alkyl)carbonyl, C₁ -C₁₀ alkenyl, C₁ -C₁₀ alkynyl, C₃ -C₁₀ cycloalkyl, C₃ -C₁₀ cycloalkylalkyl, aryl(C₁ -C₆ alkyl)-, heteroaryl(C₁ -C₆ alkyl)-, aryl, heteroaryl, CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, SO₂ R¹⁷, or SO₂ NR¹⁷ R²⁰, provided that any of the above alkyl, cycloalkyl, aryl or heteroaryl groups may optionally be substituted independently with 0-2 R¹¹ ; Y is selected from:--COR¹⁹, --SO₃ H, --PO₃ H, tetrazolyl, --CONHNHSO₂ CF₃, --CONHSO₂ R¹⁷, --CONHSO₂ NHR¹⁷, --NHCOCF₃, --NHCONHSO₂ R¹⁷, --NHSO₂ R¹⁷, --OPO₃ H₂, --OSO₃ H, --PO₃ H₂, --SO₃ H, --SO₂ NHCOR¹⁷, --SO₂ NHCO₂ R¹⁷, ##STR38## R¹⁶ is selected from: --N(R²⁰)--C(═O)--O--R¹⁷, --N(R²⁰)--C(═O)--R¹⁷, --N(R²⁰)--C(═O)--NH--R¹⁷, --N(R²⁰)SO₂ --R¹⁷, or --N(R²⁰)SO₂ --NR²⁰ R¹⁷ ; R¹⁷ is selected from:C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl) heteroaryl, arylaryl (C₁ -C₆ alkyl)-, heteroarylaryl (C₁ -C₆ alkyl)-, arylheteroaryl (C₁ -C₆ alkyl)-, heteroarylheteroaryl (C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ; R¹⁸ is selected from:H, --C(═O)--O--R¹⁷, --C(═O)--R¹⁷, --C(═O)--NH--R¹⁷, --SO₂ --R¹⁷, or --SO₂ --NR²⁰ R¹⁷ ; R¹⁹ is selected from:hydroxy, C₁ -C₁₀ alkyloxy, C₃ -C₁₁ cycloalkyloxy, aryloxy, aryl(C₁ -C₆ alkoxy)-, C₃ -C₁₀ alkylcarbonyloxyalkyloxy, C₃ -C₁₀ alkoxycarbonyloxyalkyloxy, C₂ -C₁₀ alkoxycarbonylalkyloxy, C₅ -C₁₀ cycloalkylcarbonyloxyalkyloxy, C₅ -C₁₀ cycloalkoxycarbonyloxyalkyloxy, C₅ -C₁₀ cycloalkoxycarbonylalkyloxy, C₇ -C₁₁ aryloxycarbonylalkyloxy, C₈ -C₁₂ aryloxycarbonyloxyalkyloxy, C₈ -C₁₂ arylcarbonyloxyalkyloxy, C₅ -C₁₀ alkoxyalkylcarbonyloxyalkyloxy, C₅ -C₁₀ (5-alkyl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, C₁₀ -C₁₄ (5-aryl-1,3-dioxa-cyclopenten-2-one-yl)methyloxy, or (R¹¹) (R¹²)N--(C₁ -C₁₀ alkoxy)-; R²⁰ selected from: H, C₁ -C₆ alkyl, C₃ -C₇ cycloalkyl, C₄ -C₁₁ cycloalkylalkyl, aryl, aryl(C₁ -C₆ alkyl)-, or heteroaryl (C₁ -C₆ alkyl)-; m is 1-2; n is 0-2; p is 0-2; q is 0-2; and r is 0-2;provided that: n, q, and r are chosen such that the number of in-chain atoms between R¹ and Y is in the range of 8-18.
 3. A compound of claim 1 of the Formula I and pharmaceutically acceptable salt forms thereof wherein:Q is selected from: ##STR39## R¹ is selected from: ##STR40## wherein the above heterocycles are optionally substituted with 0-2 substituents selected from the group consisting of: NH₂, halogen, NO₂, CN, CF₃, C₁ -C₄ alkoxy, C₁ -C₆ alkyl, and C₃ -C₇ cycloalkyl; R² is selected from: H, C₁ -C₄ alkyl or benzyl; U is --NH(CH₂)_(n) --; V is --(CH₂)_(n) --; R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl; W is --C(═O)--N(R¹³)--; X is --CH(R¹⁴)--CH(R¹⁵)--; R¹³ is H or CH₃ ; R¹⁴ is selected from:H, C₁ -C₁₀ alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ; R¹⁵ is H or R¹⁶ ; Y is --C(═O)R¹⁹ ; R¹⁶ is selected from:--N(R²⁰)--C(═O)--O--R¹⁷, --N(R²⁰)--C(═O)--R¹⁷, --N(R²⁰)--C(═O)--NH--R¹⁷, --N(R²⁰)SO₂ --R¹⁷, or --N(R²⁰)SO₂ --N(R²⁰)R¹⁷ ; R¹⁷ is selected from:C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl (C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl) heteroaryl, arylaryl (C₁ -C₆ alkyl)-, heteroarylaryl (C₁ -C₆ alkyl)-, arylheteroaryl (C₁ -C₆ alkyl)-, heteroarylheteroaryl (C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ; R¹⁹ is selected from:hydroxy, C₁ -C₁₀ alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R²⁰ is H or CH₃ ; and n is 0-1.
 4. A compound of claim 1 of the Formula I and pharmaceutically acceptable salt forms thereof wherein:Q is selected from: ##STR41## R¹ is selected from: ##STR42## R² is selected: H, C₁ -C₄ alkyl, or benzyl; U is --NH(CH₂)_(n) --; V is --(CH₂)_(n) --; R¹⁰ is selected from: H, CO₂ R¹⁷, C(═O)R¹⁷, C(═O)NR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R^(10a) is selected from: CO₂ R¹⁷, C(═O)R¹⁷, CONR¹⁷ R²⁰, --SO₂ R¹⁷, --SO₂ NR¹⁷ R²⁰, C₁ -C₆ alkyl substituted with 0-1 R¹⁵, C₃ -C₆ alkenyl substituted with 0-1 R¹⁵, C₃ -C₇ cycloalkyl substituted with 0-1 R¹⁵, C₄ -C₁₁ cycloalkylalkyl substituted with 0-1 R¹⁵, aryl substituted with 0-1 R¹⁵ or 0-2 R¹¹, or aryl(C₁ -C₆ alkyl)- substituted with 0-1 R¹⁵ or 0-2 R¹¹ ; R¹¹ is selected from H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, aryl(C₁ -C₆ alkyl)-, (C₁ -C₄ alkoxy)carbonyl, (C₁ -C₄ alkyl)carbonyl, C₁ -C₄ alkylsulfonyl, or C₁ -C₄ alkylaminosulfonyl; W is --C(═O)--N(R¹³)--; X is --CH(R¹⁴)--CH(R¹⁵) R¹³ is H or CH₃ ; R¹⁴ is selected from:H, C₁ -C₁₀ alkyl, aryl, or heteroaryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ; R¹⁵ is H or R¹⁶ ; Y is --C(═O)R¹⁹ ; R¹⁶ is selected from:--N(R²⁰)--C(═O)--O--R¹⁷, --N(R²⁰)--C(═O)--R¹⁷, --N(R²⁰) SO₂ --R¹⁷, R¹⁷ is selected from:C₁ -C₁₀ alkyl, C₃ -C₁₁ cycloalkyl, aryl (C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl)aryl, heteroaryl(C₁ -C₆ alkyl)-, (C₁ -C₆ alkyl) heteroaryl, arylaryl (C₁ -C₆ alkyl)-, heteroarylaryl (C₁ -C₆ alkyl)-, arylheteroaryl (C₁ -C₆ alkyl)-, heteroarylheteroaryl (C₁ -C₆ alkyl)-, heteroaryl, or aryl, wherein said aryl or heteroaryl groups are optionally substituted with 0-3 substituents independently selected from the group consisting of: C₁ -C₄ alkyl, C₁ -C₄ alkoxy, aryl, halo, cyano, amino, CF₃, and NO₂ ; R¹⁹ is selected from:hydroxy, C₁ -C₁₀ alkoxy, methylcarbonyloxymethoxy-, ethylcarbonyloxymethoxy-, t-butylcarbonyloxymethoxy-, cyclohexylcarbonyloxymethoxy-, 1-(methylcarbonyloxy)ethoxy-, 1-(ethylcarbonyloxy)ethoxy-, 1-(t-butylcarbonyloxy)ethoxy-, 1-(cyclohexylcarbonyloxy)ethoxy-, i-propyloxycarbonyloxymethoxy-, t-butyloxycarbonyloxymethoxy-, 1-(i-propyloxycarbonyloxy)ethoxy-, 1-(cyclohexyloxycarbonyloxy)ethoxy-, 1-(t-butyloxycarbonyloxy)ethoxy-, dimethylaminoethoxy-, diethylaminoethoxy-, (5-methyl-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (5-(t-butyl)-1,3-dioxacyclopenten-2-on-4-yl)methoxy-, (1,3-dioxa-5-phenyl-cyclopenten-2-on-4-yl)methoxy-, or 1-(2-(2-methoxypropyl)carbonyloxy)ethoxy-; R²⁰ is H or CH₃ ; and n is 0-1.
 5. A compound of claim 1 and enantiomeric or diasteriomeric forms thereof, or mixtures of enantiomeric or diastereomeric forms thereof, and pharmaceutically acceptable salt forms thereof, selected from the group consisting of:(S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (3,5-dimethylisoxazol4-yl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 8- (6-aminopyridin-2-yl)methyl!-!-1-oxa-2,8-diazaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 8- (6-aminopyridin-2-yl)methyl!!-1-oxa-2,8-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 8- 2-(4,5-dihydroimidazol-2-yl)aminomethyl!-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!-propionic acid, (S)-2- (2-methylphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-chloro-4-methylphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (4-biphenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-bromophenyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (1-naphthyl)sulfonyl!amino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid (S)-2-phenylsulfonylamino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2- biphenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-!-1-oxa-2-azaspiro- 4,5!-dec-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- biphenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- biphenylsulfonyl!amino-3- 8-(2-imidazolylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- biphenylsulfonyl!amino-3-( 7-benzyloxycarbonyl-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 7-benzyloxycarbonyl-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- biphenylsulfonyl!amino-3- 7-benzyloxycarbonyl-8-8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-phenylsulfonylamino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2-benzyloxycarbonylamino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethylphenyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dichlorophenyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2,6-dimethyl-4-phenyl)phenylsulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- (2-naphthyl)sulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, (S)-2- biphenylsulfonyl!amino-3- 8-(4,5-dihydroimidazol-2-yl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid, and (S)-2- (2,4,6-trimethylphenyl)sulfonyl!amino-3- 8-(2-benzimidazolyl)aminomethyl-1-oxa-2,7-diazaspiro- 4,4!-non-2-en-3-yl!carbonylamino!propionic acid.
 6. A method for the treatment of cancer metastasis, diabetic retinopathy, neovascular glaucoma, thrombosis, restenosis, osteoporosis, or macular degeneration which comprises administering to a host in need of such treatment a therapeutically effective amount of a compound of claim any one of claims 1-5.
 7. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of any one of claims 1-5. 